cas 7250-94-4, 2-ACETOXYACETOPHENONE | Articles data

Articles about 7250-94-4Total 61 be found

Article title
Article abstract
Author
Journal number and time
Download

Thermal and bromide ion-catalyzed rearrangement of benzofuran dioxetanes to 1-oxaspiro[2.5]octa-5,7-dien-4-ones
The reaction of the tetrasubstituted benzofuran dioxetanes 2 with various nucleophiles, e.g. Br-, Cl-, I-, and HN(i-Pr)2, was investigated and the unprecedented bromide ion-catalyzed rearrangement to the hithert
Adam, Waldemar,Ahrweiler, Michael,Reinhard, Dirk
p. 6713 - 6718
(1994)
Read Online

A medicinal composition for combining thioxanthone paclitaxel and STAT3 inhibitor
A medicinal composition for combining thioxanthone paclitaxel and STAT3 inhibitor, comprising an active ingredient and a pharmaceutically acceptable adjuvant, characterized in that the active ingredient is composed of paclitaxel and a STAT3 inhibitor represented by formula (I) (shown in the description), and the mass ratio of the paclitaxel to the STAT3 inhibitor represented by formula (I) in theactive ingredient is (0.18 to 0.32): 1. The compound has an effect on MDA having persistently activated STAT3 activity-MB-468 cell, DU-145 cells had good inhibitory effect.
-
Paragraph 0043; 0044; 0045; 0046

(2019/01/23)

Medicinal composition for combination of paclitaxel and fluorene STAT3 inhibitor
The invention belongs to the field of pharmaceutical chemistry, and relates to a medicinal composition for combination of paclitaxel and fluorene STAT3 inhibitors. The medicinal composition comprisesan active ingredient consisting of paclitaxel and a STAT3 inhibitor represented by formula (I), and a pharmaceutically acceptable adjuvant, wherein the mass ratio of the paclitaxel to the STAT3 inhibitor represented by formula (I) in the active ingredient is (0.27 to 0.39): 1. The compound has an effect on having persistently activated STAT3 activity MDA-MB-468 cell, DU-145 cells had good inhibitory effect.
-
Paragraph 0045-0048

(2019/02/04)

A carbazole class STAT inhibitors maleic acid salt crystal form II combination pharmaceutical composition and its preparation method
The invention belongs to the field of medicinal chemistry, and in particular relates to with tumor compound of 4 - (9 - ethyl - 9 H - carbazole - 4 - yl) - 6 - (4 - aminophenyl alkene propionyl) - N - (2 - methyl - 4 H - chromene - 4 - keto) - 1, 3, 5 - triazine - 2 - amine maleic acid salt of a new crystalline form, its preparation method, comprising the composition of said form, said form and said form or comprise the composition of use in the preparation of the medicament, the crystalline form II has good physical and chemical stability, solubility and bioavailability, is suitable for formulation development.
-
Paragraph 0039-0042

(2019/02/13)

STAT3 inhibitors and application thereof
The invention belongs to the field of medical chemistry, relates to STAT3 inhibitors and an application thereof and particularly relates to compounds for inhibiting the signal transduction and transcription activator-3, a pharmaceutical composition containing the compound and a use of the compounds or the pharmaceutical composition as cancer treatment drugs. The compounds can well inhibit MDA-MB-468 cells and DU-145 cells with sustained STAT3 activity.
-
Paragraph 0037-0040

(2019/01/20)

Preparation method of STAT3 inhibitor
The invention belongs to the field of medical chemistry, relates to a class-I STAT3 inhibitor and an application thereof, and particularly relates to a method for preparing compounds having signal transduction and transcriptional activator 3 inhibitory effects. The compounds can well inhibit MDA-MB-468 cells and DU-145 cells with continuous STAT3 activity.
-
Paragraph 0047-0050

(2019/01/23)

A fluorene STAT3 inhibitor and its preparation method
The invention belongs to the field of medicinal chemistry, relates to a compound of formula (I) of fluorene STAT3 inhibitor and its application, in particular to a kind of with signal conduction with a transcription activating factor - 3 inhibiting effect of a compound, pharmaceutical composition containing the compound, and the compound or pharmaceutical composition as the use of the cancer therapy, the compounds with sustained activation of STAT3 activity of MDA - MB - 468 cell, DU - 145 cell good inhibition effect.
-
Paragraph 0044-0047

(2019/02/13)

Combined pharmaceutical composition of paclitaxel and dibenz [b, d] thiophene STAT inhibitor tartrate
The invention provides a combined pharmaceutical composition of paclitaxel and dibenz [b, d] thiophene STAT inhibitor tartrate, comprising active ingredients and pharmaceutically acceptable excipients. The active ingredient consists of paclitaxel and dibenz [b, d] thiophene STAT inhibitor tartrate represented by formula (I), and the mass ratio of paclitaxel to dibenz [b, d] thiophene STAT inhibitor tartrate represented by formula (I) in the active ingredient is (0.09 to 0.21): 1. A tartrate salt in that composition has good water solubility, high bioavailability and good stability.
-
Paragraph 0027-0030

(2019/01/24)

A medicinal composition for combine paclitaxel and fluorenone STAT3 inhibitor
Disclosed is a medicinal composition for combine paclitaxel and fluorenone STAT3 inhibitor comprising an active ingredient and a pharmaceutically acceptable adjuvant, characterized in that the activeingredient is composed of paclitaxel and a STAT3 inhibitor represented by formula (I), and the mass ratio of the paclitaxel to the STAT3 inhibitor represented by formula (I) in the active ingredient is (0.21 to 0.32): 1. The compound has an effect on MDA having persistently activated STAT3 activity-MB-468 cell, DU-145 cells had good inhibitory effect.
-
Paragraph 0042-0045

(2019/01/24)

A paclitaxel and carbazole class STAT3 inhibitor crystalline form A combination pharmaceutical composition
The present invention provides a kind of paclitaxel and carbazole class STAT3 inhibitor crystalline form A combination pharmaceutical composition, comprising an active ingredient and a pharmaceutically acceptable auxiliary material, characterized in that the by the taxol the active ingredient of the formula (I) indicated by the STAT3 inhibitors A a crystalline form, the active ingredient of taxol in the formula (I) indicated by the STAT3 inhibitors the mass ratio of the crystalline form A (0.09 - 0.21): 1. The A crystalline form has good physical and chemical stability, solubility and bioavailability, suitable for formulation development.
-
Paragraph 0029; 0040-0042

(2019/02/13)

Indoles STAT3 (Signal Transducer and Activator of Transcription-3) inhibitor and preparation method thereof
The invention belongs to the field of medical chemistry, and relates to an STAT3 (Signal Transducer and Activator of Transcription-3) inhibitor represented by the formula (I) and a preparation methodand application thereof, in particular to a compound having a STAT3 inhibition effect, a pharmaceutical composition containing the compound, and use of the compound or pharmaceutical composition as atherapeutic drug for cancers. The compound has a good inhibition effect on MDA-MB-468 cells and DU-145 cells which have sustainably activated STAT3 activity.
-
Paragraph 0038-0041

(2019/02/27)

Mesylate of STAT3 inhibitor as well as preparation method and application thereof
The invention belongs to the field of medicinal chemistry and relates to mesylate of a STAT3 inhibitor as well as a preparation method and application thereof. Particularly, the invention relates to mesylate of 4-(9-ethyl-9H-carbazole-4-yl)-6-(4-allylaminophenyl)-N-(2-methyl-4H-chromene-4-one)-1,3,5-triazine-2-amine as well as a preparation method and application thereof. The structure of the mesylate of 4-(9-ethyl-9H-carbazole-4-yl)-6-(4-allylaminophenyl)-N-(2-methyl-4H-chromene-4-one)-1,3,5-triazine-2-amine is as shown in the description. The mesylate is excellent in water solubility, high in bioavailability and excellent in stability.
-
Paragraph 0027; 0028-0033

(2019/02/27)

Dibenzo [b, d] thiophene STAT3 inhibitors of M crystal form and its preparation method
The invention belongs to the field of medicinal chemistry, with tumor specific relates to the effect of a compound 4 - (dibenzo [b, d] thiophene - 4 - yl) - 6 - (4 - aminophenyl alkene propionyl) - N - (2 - methyl - 4 H - chromene - 4 - keto) - 1, 3, 5 - triazine - 2 - deferoxamine mesylate salt of a new crystalline form, its preparation method, comprising the composition of said form, said form and said form or comprise the composition of use in the preparation of the medicament, the A crystalline form has good physical and chemical stability, solubility and bioavailability, is suitable for formulation development.
-
Paragraph 0042-0045

(2019/02/13)

Carbazole STAT3 inhibitor crystal form I and preparation method thereof
The invention belongs to the field of medical chemistry and particularly relates to a novel crystal form of a compound 4-(9-ethyl-9H-carbazole-4)-6-(4-acrylyl aminophenyl)-N-(2-methyl-4H-chromene-4-ketone)-1,3,5-triazine-2-amine maleate with an anti-tumor effect, a preparation method of the novel crystal form, a composition comprising the crystal form, and an application of the crystal form or thecomposition comprising the crystal form in medicine preparation. The crystal form I has good physical and chemical stability, solubility and bioavailability and is suitable for preparation development.
-
Paragraph 0032; 0043-0046

(2019/02/27)

Crystal form A of fluorenone STAT3 inhibitor and preparation method
The invention belongs to the field of medical chemistry, relates to a fluorenone STAT3 inhibitor represented by a formula (I) and an application thereof and particularly relates to a compound with a signal transduction effect and an inhibition effect on a transcriptional activation factor-3, a pharmaceutical composition containing the compound and use of the compound or the pharmaceutical composition as a cancer treatment drug. The compound has good inhibition effect to MDA-MB-468 cells and DU-145 cells which have continuously-activated STAT3 activity.
-
Paragraph 0049; 0050-0052

(2019/03/06)

Carbazole class STAT3 inhibitor crystalline form A and its preparation method (by machine translation)
The invention belongs to the field of medicinal chemistry, and in particular relates to with tumor compound of 4 - (9 - ethyl - 9 H - carbazole - 4 - yl) - 6 - (4 - aminophenyl alkene propionyl) - N - (2 - methyl - 4 H - chromene - 4 - keto) - 1, 3, 5 - triazine - 2 - deferoxamine mesylate salt of a new crystalline form, its preparation method, comprising the composition of said form, said form and said form or comprise the composition of use in the preparation of the medicament, the A crystalline form has good physical and chemical stability, solubility and bioavailability, is suitable for formulation development. (by machine translation)
-
Paragraph 0031; 0042-0045

(2019/02/27)

Maleate of STAT3 inhibitor as well as preparation method and application thereof
The invention belongs to the field of medicinal chemistry and relates to maleate of a STAT3 inhibitor as well as a preparation method and application thereof. Particularly, the invention relates to maleate of 4-(9-ethyl-9H-carbazole-4-yl)-6-(4-allylaminophenyl)-N-(2-methyl-4H-chromene-4-one)-1,3,5-triazine-2-amine as well as a preparation method and application thereof. The structure of the maleate of 4-(9-ethyl-9H-carbazole-4-yl)-6-(4-allylaminophenyl)-N-(2-methyl-4H-chromene-4-one)-1,3,5-triazine-2-amine is as shown in the description. The maleate is excellent in water solubility, high in bioavailability and excellent in stability.
-
Paragraph 0027-0030

(2019/02/27)

Crystal form P of carbazole STAT3 inhibitor and preparation method of crystal form P
The invention belongs to the field of medical chemistry and particularly relates to a novel crystal form of a compound 4-(9-ethyl-9H-carbazole-4-yl)-6-(4-allylaminophenyl)-N-(2-methyl-4H-chromen-4-one)-1,3,5-triazin-2-amine methanesulfonate with an anti-tumor effect, a preparation method of the crystal form, a composition containing the crystal form and use of the crystal form or the composition containing the crystal form in the drug preparation. The crystal form P has good physical-chemical stability, solubility and bioavailability and is proper in particle size, D50 is 35-40 microns, particle distribution curves are distributed in a normal single-peak manner, and the crystal form is suitable for preparation development.
-
Paragraph 0044-0047

(2019/03/06)

Paclitaxel and dibenzo[b,d]thiophene STAT (Signal Transducer and Activator of Transcription) inhibitor mesylate A crystal form combined pharmaceutical composition
The invention provides a paclitaxel and dibenzo[b,d]thiophene STAT (Signal Transducer and Activator of Transcription) inhibitor mesylate A crystal form combined pharmaceutical composition, comprisingan active ingredient and a pharmaceutically acceptable excipient, and characterized in that: the active ingredient is composed of paclitaxel and dibenzo[B,D]thiophene STAT inhibitor mesylate A represented by the formula (I); a mass ratio of the paclitaxel to the dibenzo[B,D]thiophene STAT inhibitor mesylate A in the active ingredient is (0.09-0.21):1. The A crystal form has good physical and chemical stability, solubility and bioavailability, and is suitable for development of preparations.
-
Paragraph 0029; 0041-0044

(2019/02/27)

Crystal form II of carbazole STAT3 inhibitor and preparation method of crystal form II
The invention belongs to the field of medical chemistry and particularly relates to a novel crystal form of a compound 4-(9-ethyl-9H-carbazole-4-yl)-6-(4-allylaminophenyl)-N-(2-methyl-4H-chromen-4-one)-1,3,5-triazin-2-amine maleate with an anti-tumor effect, a preparation method of the crystal form, a composition containing the crystal form and use of the crystal form or the composition containingthe crystal form in the drug preparation. The crystal form II has good physical-chemical stability, solubility and bioavailability and is suitable for preparation development.
-
Paragraph 0040-0043

(2019/03/06)

Tartrate of dibenzo[b,d]thiophene STAT3 (Signal Transducer and Activator of Transcription-3) inhibitor and preparation method and application of tartrate
The invention belongs to the field of pharmaceutical chemistry, and relates to tartrate of a dibenzo[b,d]thiophene STAT3 (Signal Transducer and Activator of Transcription-3) inhibitor and a preparation method and application of the tartrate, particularly, the invention relates to the tartrate of 4-(dibenzo[b,d]thiophene-4-yl)-6-(4-allyl acylamino phenyl)-N-(2-methyl-4H-chromene-4-keto)-1,3,5-triazine-2-amine and the preparation method and the application of the tartrate, the structure of the tartrate of 4-(dibenzo[b,d]thiophene-4-yl)-6-(4-allyl acylamino phenyl)-N-(2-methyl-4H-chromene-4-keto)-1,3,5-triazine-2-amine is shown in the description, and the tartrate is good in water solubility, high in bioavailability and good in stability.
-
Paragraph 0028; 0029; 0030; 0031

(2019/02/27)

Dibenzo [b, d] thiophene STAT3 inhibitors of a sulfonate and its preparation method and use thereof (by machine translation)
The invention belongs to the field of pharmaceutical chemistry, relates to dibenzo [b, d] thiophene STAT3 inhibitors of a sulfonate and its preparation method and use thereof, in particular, the invention relates to 4 - (dibenzo [b, d] thiophene - 4 - yl) - 6 - (4 - aminophenyl alkene propionyl) - N - (2 - methyl - 4 H - chromene - 4 - keto) - 1, 3, 5 - triazine - 2 - amine of a sulfonate and its preparation method and use thereof, said 4 - (dibenzo [b, d] thiophene - 4 - yl) - 6 - (4 - aminophenyl alkene propionyl) - N - (2 - methyl - 4 H - chromene - 4 - keto) - 1, 3, 5 - triazine - 2 - amine mesylate salt structure is shown as follows, its methanesulfonate good water solubility, bioavailability is high, good stability. (by machine translation)
-
Paragraph 0028; 0029; 0030; 0031

(2019/02/27)

Thioxanthone Signal Transducer and Activator of Transcription-3 (STAT3) inhibitor and application thereof
The invention belongs to the field of medical chemistry, and relates to a thioxanthone Signal Transducer and Activator of Transcription-3 (STAT3) inhibitor as shown by a formula (I) and application thereof, in particular to a compound with STAT3 inhibiting effects, a drug composition containing the compound, and the application of the compound or the drug composition as a cancer treatment drug. The compound has remarkable inhibiting effects on MDA-MB-468 cells and DU-145 cells with continuously activated STAT3 activity. (The formula is as shown in the description).
-
Paragraph 0042; 0043; 0044; 0045

(2019/02/27)

A fluorenones STAT3 inhibitor and preparation method and application
The invention belongs to the field of medicinal chemistry, relates to a compound of formula (I) of the fluorenones STAT3 inhibitor and its application, in particular to a kind of with signal conduction with a transcription activating factor - 3 inhibiting effect of a compound, pharmaceutical composition containing the compound, and the compound or pharmaceutical composition as the use of the cancer therapy, the compounds with sustained activation of STAT3 activity of MDA - MB - 468 cell, DU - 145 cell good inhibition effect.
-
Paragraph 0041; 0042; 0043; 0044

(2019/04/09)

Paclitaxel and carbazole STAT inhibitor maleate crystal form I combination pharmaceutical composition
The present invention provides a paclitaxel and carbazole STAT inhibitor maleate crystal form I combination pharmaceutical composition. The composition comprises active ingredients and pharmaceutically acceptable accessory materials. The active ingredients comprise paclitaxel and a STAT inhibitor crystal form I shown in a formula (I), and a mass ratio of the paclitaxel to the STAT inhibitor crystal form I shown in the formula (I) is (0.14-0.22):1 in the active ingredients. The crystal form I has good physical and chemical stability, solubility and bioavailability, and is suitable for formulation development.
-
Paragraph 0042-0045

(2019/10/01)

Thioxanthone STAT3 (signal transducer and activator of transcription-3) inhibitor maleate crystal form A and application thereof
The invention belongs to the field of medical chemistry and relates to a thioxanthone STAT3 (signal transducer and activator of transcription-3) inhibitor shown as formula (I) and an application thereof, in particular to compounds with a STAT3 inhibition function, pharmaceutical composition containing the compounds and an application of the compounds or the pharmaceutical composition as cancer treatment drugs. The compounds have good inhibition functions on MDA-MB-468 cells and DU-145 cells with continuously activated STAT3 activity.
-
Paragraph 0046-0049

(2019/09/17)

A paclitaxel and carbazole class STAT inhibitors methanesulfonate crystalline form P combination pharmaceutical composition (by machine translation)
Books invention provides a paclitaxel and carbazole class STAT inhibitors methanesulfonate crystalline form P combination pharmaceutical composition, comprising an active ingredient and a pharmaceutically acceptable auxiliary material, wherein the active ingredient by the taxol of formula (I) indicated by the STAT3 inhibitor P a crystalline form, the active ingredient of taxol in the formula (I) indicated by the STAT3 inhibitors crystal mass ratio of P (0.09 - 0.21): 1. The P crystalline form has good physical and chemical stability, solubility and bioavailability, particle size is suitable in size, and the distribution of the particle size distribution curve of a regular [...], suitable for formulation development. (by machine translation)
-
Paragraph 0042-0045

(2019/02/13)

Novel chromone and xanthone derivatives: Synthesis and ROS/RNS scavenging activities
Chromones and xanthones are oxygen-containing heterocyclic compounds acknowledged by their antioxidant properties. In an effort to develop novel agents with improved activity, a series of compounds belonging to these chemical classes were prepared. Their syntheses involve the condensation of appropriate 2-methyl-4H-chromen-4-ones, obtained via Baker-Venkataraman rearrangement, with (E)-3-(3,4-dimethoxyphenyl)acrylaldehyde to provide the corresponding 2-[(1E,3E)-4-(3,4-dimethoxyphenyl)buta-1,3-dien-1-yl]-4H-chromen-4-ones. Subsequent electrocyclization and oxidation of these compounds led to the synthesis of 1-aryl-9H-xanthen-9-ones. After cleavage of the protecting groups, hydroxylated chromones and xanthones were assessed as scavenging agents against both reactive oxygen species (ROS) [superoxide radical (O2?-), hydrogen peroxide (H2O2), hypochlorous acid (HOCl), singlet oxygen (1O2), and peroxyl radical (ROO?)] and reactive nitrogen species (RNS) [nitric oxide (?NO) and peroxynitrite anion (ONOO-)]. Generally, all the tested new hydroxylated chromones and xanthones exhibited scavenger effects dependent on the concentration, with IC50 values found in the micromolar range. Some of them were shown to have improved scavenging activity when compared with previously reported analogues, allowing the inference of preliminary conclusions on the structure-activity relationship.
Proen?a, Carina,Albuquerque, Hélio M.T.,Ribeiro, Daniela,Freitas, Marisa,Santos, Clementina M.M.,Silva, Artur M.S.,Fernandes, Eduarda
p. 381 - 392
(2016/04/06)

SKIN WHITENING AGENT CONTAINING NOVEL CYCLIC COMPOUND
Provided is a derivative or a polyhydroxy cyclic compound represented by Formula I or a pharmacologically acceptable salt thereof with excellent whitening effects, comprising; wherein {circle around (A)} is derived from an aromatic cyclic compound, B is hydrogen, oxo (═O), amino (—NH2), imino (═NH), or a saturated or unsaturated straight or branched alkyl, alkoxy, monoalkylamino, or dialkylamino group having 1 to 10 carbon atoms, Cn, Cn+1and Cn+2 are three neighboring carbon atoms present in the aromatic cyclic compound, wherein n is a positive integer, R1 is hydrogen, hydroxy, or a saturated or unsaturated straight or branched alkyl or alkoxy group, X and Y are selected from a group consisting of hydrogen, hydroxy, and a saturated or unsaturated straight or branched alkoxy, or acyloxy group, and one of X and Y is hydrogen, R2, R3, R4 and R5 are each independently at least one substituent selected from a group consisting of hydrogen, alkyl, alkoxy, acyloxy, acyloxymethyl, oxo, hydroxy, vinyl, nitrile, carboxaldehyde, carbonitrile and aldehyde.
-
Paragraph 0152; 0153

(2016/08/29)

Synthesis and characterization of novel oxime derivatives
Background: The synthesis of effective drugs are very important for the scientist. The various biological effects of the thiazole, oxime and ether functional groups are well known properties by the drug developers. So we have synthesised new molecules which contains three of them on the same molecules. Methods: The acetophenone derivatives have been used for synthesis new oximes. The synthetic pathway includes mainly four steps. s1. α-Bromination of acetophenone derivatives, s2. Synthesis of thiazole ring using brominated acetophenones, s3. Synthesis of ethers using synthesised thiazole, s4. Synthesis of oximes. Results: The synthesised molecules characterised using IR,1H-NMR, 13C-NMR and elementel analysis methods. Conclusion: The new oximes which include thiazole and ether groups have been synthesised using acetophenone derivatives.
Arslan, Taner,Keskin, Serhat,Demirayak, Seref
p. 672 - 677
(2017/01/13)

Synthesis of Aryl Ketoamides via Aryne Insertion into Imides
An insertion of arenes into both imides and anhydrides via reactive aryne intermediates is presented. The reaction is performed under exceptionally mild conditions, and the corresponding ketoamide products are amenable to derivatization to deliver a variety of synthetically useful motifs such as quinolones, indoles, and ketoanilines.
Wright, Austin C.,Haley, Christopher K.,Lapointe, Guillaume,Stoltz, Brian M.
supporting information
p. 2793 - 2795
(2016/07/06)

One-Pot Synthesis of Benzopyran-4-ones with Cancer Preventive and Therapeutic Potential
A one-pot synthesis of novel benzopyran-4-ones is described. In a tandem reaction, organobase-catalysed Michael addition of R1COCH2COR2 on chromone-3-carboxylic acid led to decarboxylation and pyran-4-one ring opening of the latter. This was followed by chromone-and/or chromanone ring closure of the resulting Michael adducts when R1 is an ortho-hydroxyaryl group. Antioxidant testing of 14 derivatives identified strong antiradical properties of chromanones 3o-r (2.1-3.1 μmol Trolox equiv./μmol compound in the DPPH assay). Chromanones 3p and 3r and 2-styrylchromone 3k were also most potent in inducing the cytoprotective Keap1-Nrf2 signalling pathway in a reporter gene assay (fivefold induction at concentrations 3 μM). Of the seven compounds evaluated for antiproliferative activities, 3k and 3r were the most active, inhibiting leukaemia K562 cell proliferation by 50 % after 72 h at concentrations of 4.5 and 7.9 μM, whereas normal peripheral blood mononuclear cells were not affected. Chromanones 3p and 3r and 2-styrylchromones 3k potently activate the Nrf2 response in the AREc32 cell line at low micromolar concentrations (C5 3 μM). Compounds 3k and 3r are also the most active in inhibiting cell proliferation by 50 % after 72 h incubation at concentrations of 4.5 and 7.7 μM, whereas normal peripheral blood mononuclear cells were not affected.
Talhi, Oualid,Brodziak-Jarosz, Lidia,Panning, Jana,Orlikova, Barbora,Zwergel, Clemens,Tzanova, Tzvetomira,Philippot, Stéphanie,Pinto, Diana C. G. A.,Paz, Filipe A. Almeida,Gerhaüser, Clarissa,Dick, Tobias P.,Jacob, Claus,Diederich, Marc,Bagrel, Denyse,Kirsch, Gilbert,Silva, Artur M. S.
p. 965 - 975
(2016/03/01)

A near-infrared fluorescent probe for rapid detection of hydrogen peroxide in living cells
A new near-infrared and colorimetric fluorescent molecular probe was developed for rapid detection of H2O2. The near-infrared fluorescence OFF-ON switch is triggered by transformation of phenylboronic acid unit to phenol in the presence of H2O2. No quinone methides are released in this process, which is preferable for in vivo studies. In addition, probe 1 at low concentration exhibits high quality optical imaging during a short period in in vitro cell study.
Zhang, Xuan,Zhang, Lun,Liu, Yaqian,Bao, Bin,Zang, Yi,Li, Jia,Lu, Wei
p. 4842 - 4845
(2015/07/27)

New cyclic skin whiteninig agent
In the present invention, provided is a skin whitening agent, which is easily synthesized without side effects for skin and has an outstanding effect of inhibiting pigmentation on skin due to an outstanding effect of inhibiting the creation of melanine where a cyclic derivative compound or pharmaceutically acceptable salt thereof has a chemical structure in formula (I) and is accordingly used to achieve the purpose of the present invention. In the present invention, provided is a cyclic derivative compound or pharmaceutically acceptable salt thereof, which has an effect of whitening skin and a chemical structure in formula (I) where A is derived from an aromatic cyclic compound; B is derived from among hydrogen, O which is oxo, NH_2 which is amino, NH which is imino, C1-C10 of saturated or unsaturated straight or branched chain alkyl group, alkoxy, mono alkyl amino group or dialkyl amino group; and C_n, C_n+1 and C_n+2 are three neighboring carbons in the cyclic compound wherein n is a positive integer.COPYRIGHT KIPO 2015
-
Paragraph 0182-0183

(2016/11/21)

Chelating Bis-N-heterocyclic Carbene-Palladium(II) Complexes for Oxidative Arene C-H Functionalization
Bis-N-heterocyclic carbene (NHC)-chelated palladium(II) complexes have been synthesized, characterized fully including single-crystal X-ray structural analyses, and utilized for the first time toward catalytic oxidative C-H functionalization of arenes with PhI(OAc)2 and N-bromosuccinimide. (Figure Presented).
Desai, Sai Puneet,Mondal, Moumita,Choudhury, Joyanta
p. 2731 - 2736
(2015/06/30)

Synthesis, docking study and relaxant effect of 2-alkyl and 2-naphthylchromones on rat aorta and guinea-pig trachea through phosphodiesterase inhibition
Chromone (4), which form the base structure of various flavonoids isolated as natural products, is capable of relaxing smooth muscle. This is relevant to the treatment of high blood pressure, asthma and chronic obstructive pulmonary disease. The former disorder involves the contraction of vascular smooth muscle (VSM), and the latter two bronchoconstriction of airway smooth muscle (ASM). One of the principal mechanisms by which flavonoids relax muscle tissue is the inhibition of phosphodiesterases (PDEs), present in both VSM and ASM. Therefore, a study was designed to analyze the structure-activity relationship of chromone derivatives in vaso- and bronchorelaxation through the inhibition of PDE. Docking studies showed that these chromones bind at the catalytic site of PDEs. Consequently, we synthesized analogs of chromones substituted at position C-2 with alkyl and naphthyl groups. These compounds were synthesized from 2-hydroxyacetophenone and acyl chlorides in the presence of DBU and pyridine, modifying the methodology reported for the synthesis of 3-acylchromones by changing the reaction temperature from 80 to 30°C and using methylene chloride as solvent, yielding the corresponding phenolic esters 10a-10h. These compounds were cyclized with an equivalent of DBU, pyridine as solvent, and heated at reflux temperature, yielding the chromones 11a-11h. Evaluation of the vasorelaxant effect of 4, 11a-11h on rat aorta demonstrated that potency decreases with branched alkyl groups. Whereas the EC50 of compound 11d (substituted by an n-hexyl group) was 8.64 ± 0.39 μM, that of 11f (substituted by an isobutyl group) was 14.58 ± 0.64 μM. Contrarily, the effectiveness of the compound is directly proportional to the length of the alkyl chain, as evidenced by the increase in maximal effect of compound 11c versus 11d (66% versus 100%) and 11e versus 11f (60% versus 96%). With an aromatic group like naphthyl as the C-2 substituent, the effectiveness was only 43%. All compounds tested on guinea pig trachea showed less than 55% effectiveness. Compounds 4, 11a-11h were evaluated as PDE inhibitors in vitro, with 11d showing the greatest effect (73%), corroborating the importance of a long alkyl chain, which inhibits the decomposition of cGMP. Docking studies showed that the compound 11d was selective for the inhibition of PDE-5.
Rodriguez-Ramos, Fernando,Navarrete, Andres,Gonzalez-Andrade, Martin,Alarcon, Carlos,Aguilera-Cruz, Alejandro,Reyes-Ramirez, Adelfo
p. 17 - 25
(2013/10/22)

Short communication: Titanium-induced synthesis of benzofurans
Ketoesters derived from the acylation of o-hydroxyacetophenone with aliphatic as well as aromatic acid chlorides undergo intramolecular cyclization in the presence of low-valent titanium to afford benzofurans in good yields. The reduction of titanium trichloride with dry zinc powder in refluxing THF takes place in the presence of the ketoester which simultaneously cyclizes as the titanium catalyst is formed, rendering the pre-reduction of titanium trichloride in a separate step unnecessary.
Jumbam,Yedwa,Masamba
experimental part
p. 157 - 160
(2012/05/20)

Synthesis of novel 1-aryl-9 H -xanthen-9-ones
A novel route for the synthesis of 1-aryl-9H-xanthen-9-ones is reported. This methodology involves the condensation of 2-methylchromone with cinnamaldehydes leading to (E,E)-2-(4-arylbuta-1,3-dien-1-yl)-4H-chromen-4-ones. The final steps involved electrocyclization and oxidation of the latter compounds, in an one-pot synthesis, giving the desired 1-aryl-9H-xanthen-9-ones. Georg Thieme Verlag Stuttgart - New York.
Esteves, Cátia I. C.,Santos, Clementina M. M.,Brito, Cristela M.,Silva, Artur M. S.,Cavaleiro, José A. S.
scheme or table
p. 1403 - 1406
(2011/08/03)

Candida tenuis xylose reductase catalysed reduction of acetophenones: The effect of ring-substituents on catalytic efficiency
The catalytic efficiencies of Candida tenuis xylose reductase catalysed reductions of mono-substituted acetophenones are in reasonable correlation with the σ-Hammett coefficients of the substituted phenyl groups. Variations of the substrate transformation rates are hence mainly caused by mesomeric and inductive effects of the substituents, while differences in substrate binding have a secondary relevance. Some substrate 1H NMR chemical shifts and carbonyl IR absorption bands are in reasonable accordance with the catalytic activities and allow the estimation of the transformation rates with good accuracy. The resulting substituted (S)-1-phenyl ethanols are generated in very high enantiomeric excess.
Vogl, Michael,Kratzer, Regina,Nidetzky, Bernd,Brecker, Lothar
experimental part
p. 5863 - 5870
(2011/09/30)

One-pot greener protocol for the synthesis of substituted coumarins
An expeditious one-pot procedure for the synthesis of substituted coumarins under microwave irradiation is accounted. The method describes an easy and fast method for the synthesis of substituted acetoxy coumarins which are very good fluorophores for medical as well as industrial applications. It makes use of easily available reagents such as triethylamine and acetic anhydride as catalyst. The method finds good applications for the synthesis of multisubstituted coumarins.
Ranjith, Choorikkat,Paul, Nidhin,Vijayan
experimental part
p. 235 - 238
(2011/11/30)

Acetylation of alcohols and phenols with acetic anhydride under solvent-free conditions using an ionic liquid based on morpholine as a recoverable and reusable catalyst
Rapid and efficient acetylation of alcohols and phenols with acetic anhydride is performed in the presence of economical Bronsted acidic ionic liquids that bear a propanesulfonic acid group on a morpholinium cation as catalysts under solvent-free conditions. [MMPPA][HSO4] (N-methylmorpholinium propanesulfonic acid ammonium hydrogensulfate) was proven to be the most active catalyst, and after removal of water, it could be recycled and reused for up to four times without a noticeable decrease in catalytic activity. Springer-Verlag 2010.
Yue, Caibo,Liu, Qingqing,Yi, Tingfeng,Chen, Yun
experimental part
p. 975 - 978
(2011/09/30)

A TFAA-H3PO4-mediated direct, metal-free and high-speed synthesis of aryl carboxylate esters from phenols
An operationally simple, mild and single-step method for the direct and metal-free synthesis of aryl carboxylate esters is described under a solvent free condition. The reaction of phenols including 2-naphthol (or 1-naphthol) with a variety of carboxylic acids in the presence of TFAA and 85% H3PO4 provided a range of aryl carboxylate esters in good yields within few minutes.
Kankanala, Kavitha,Reddy, Vangala Ranga,Mukkanti, Khagga,Pal, Sarbani
experimental part
p. 505 - 508
(2009/12/26)

Counterattack mode differential acetylative deprotection of phenylmethyl ethers: Applications to solid phase organic reactions
A counterattack protocol for differential acetylative cleavage of phenylmethyl ether has been developed. The phenylmethyl moiety is liberated as benzyl bromide that is isolated and reused providing advantages in terms of waste minimization/utilization and atom economy. The applicability of this methodology has been extended for solid phase organic reactions with the feasibility of reuse of the solid support.
Chakraborti, Asit K.,Chankeshwara, Sunay V.
supporting information; experimental part
p. 1367 - 1370
(2009/07/04)

Molecular iodine in isopropenyl acetate (IPA): a highly efficient catalyst for the acetylation of alcohols, amines and phenols under solvent free conditions
Iodine in isopropenyl acetate (IPA) is a highly efficient catalyst for the acetylation of a variety of alcohols, phenols and amines under solvent free conditions. Primary, secondary, tertiary alcohols, amines and mono to polyhydroxy phenols and anilines with electron donating or withdrawing substituents can be easily acetylated in good to excellent yield at 85-90 °C.
Ahmed, Naseem,van Lier, Johan E.
p. 5345 - 5349
(2007/10/03)

NOVEL IMIDAZOLE COMPOUND AND USAGE THEREOF
A water-based composition for treating copper or copper alloy surface for lead-free soldering, the composition comprising a compound represented by general formula (1): wherein R1 is hydrogen or methyl, and either R2 and R3/sup
-
(2008/06/13)

New synthesis of 2,3-diarylxanthones
A new synthesis for 2,3-diarylxanthones is described. This was accomplished by aldol condensation of 3-bromo-2-methylchromone with benzaldehydes leading to the formation of 3-bromo-2-styrylchromones, followed by Heck reaction with styrenes. Georg Thieme V
Santos, Clementina M. M.,Silva, Artur M. S.,Cavaleiro, José A. S.
p. 3095 - 3098
(2007/10/03)

Facile catalyzed acylation of alcohols, phenols, amines and thiols based on ZrOCl2·8H2O and acetyl chloride in solution and in solvent-free conditions
Acylation of heteroatoms (O, N and S) with acetyl chloride based on the use of a catalytic amount of the moisture stable, inexpensive ZrOCl 2?8H2O, proceeds efficiently producing the corresponding acylated products in excellent yields.
Ghosh, Rina,Maiti, Swarupananda,Chakraborty, Arijit
p. 147 - 151
(2007/10/03)

Facile catalyzed acylation of heteroatoms using BiCl3 generated in situ from the procatalyst BiOCl and acetyl chloride
Acylation of a variety of alcohols, phenols, aliphatic and aromatic amines, a thiol and a thiophenol proceeds efficiently using BiCl3 generated in situ from the procatalyst BiOCl and acetyl chloride in a solvent or under solventless conditions, furnishing the corresponding acylated derivatives in very good to excellent yields.
Ghosh, Rina,Maiti, Swarupananda,Chakraborty, Arijit
p. 6775 - 6778
(2007/10/03)

Copper(II) Tetrafluoroborate-Catalyzed Acetylation of Phenols, Thiols, Alcohols, and Amines
Copper(II) tetrafluoroborate efficiently catalyzes acetylation of structurally diverse phenols, alcohols, thiols, and amines with stoichiometric amounts of Ac2O under solvent-free conditions at room temperature. Acid-sensitive alcohols are smoothly acetylated without competitive side reactions. The reaction is influenced by the steric and electronic factors associated with the substrate as well as the anhydride. Acetylation of a sterically hindered substrate requires excess of anhydride and longer time. Acylation with less electrophilic anhydrides affords poor to moderate yields.
Chakraborti, Asit K.,Gulhane, Rajesh,Shivani
p. 111 - 115
(2007/10/03)

Electrostatic catalysis by ionic aggregates: Scope and limitations of Mg(ClO4)2 as acylation catalyst
Alkali and alkaline earth metal perchlorates exhibit electrostatic catalysis in the activation of anhydrides for the acylation reaction. Perchlorates with higher values of the charge-size function of the metal ion exhibit better catalytic activity following the order Mg(ClO4) 2>Ba(ClO4)2>LiClO4. Acylation of structurally diverse phenols, thiols, alcohols, and amines have been carried out with stoichiometric amounts of anhydride at room temperature under solvent free conditions in the presence of catalytic amount of Mg(ClO4) 2. Sterically hindered and electron deficient phenols are efficiently acylated. Acylation with sterically hindered anhydrides such as iso-butyric, pivalic, and benzoic anhydrides are carried out with phenols and alcohols in excellent yields. Acid-sensitive alcohols are acylated in excellent yields without any competitive side reactions.
Chakraborti, Asit K.,Sharma, Lalima,Gulhane, Rajesh,Shivani
p. 7661 - 7668
(2007/10/03)

Bismuth Oxide Perchlorate as a Highly Efficient Catalyst for Heteroatom Acylation under Solvent-Free Conditions
Bismuth oxide perchlorate efficiently catalyzes the acetylation of structurally diverse phenols, alcohols, thiols, and amines under solvent free conditions. Sterically hindered and electron deficient phenols are acetylated in excellent yields with stoichiometric amounts of Ac2O at room temperature. Acylation of acid-sensitive alcohols is carried out efficiently without competitive side reactions. Optically active substrates are acetylated without any detrimental effect on the optical purity.
Chakraborti, Asit K.,Gulhane, Rajesh,Shivani
p. 1805 - 1808
(2007/10/03)