- New cyclometalated iridium(III) dye chromophore complexes for p-type dye-sensitised solar cells
-
The synthesis of seven iridium complexes [Ir(C?N)2(N?N)][PF6] (AS9-15) designed as dyes for p-type DSSC is described. These complexes comprise a 4-(pyrid-2-yl)benzoic acid as the cyclometalating/anchoring ligand with different diimin
- Sinopoli, Alessandro,Wood, Christopher J.,Gibson, Elizabeth A.,Elliott, Paul I.P.
-
-
Read Online
- Photo-induced deep aerobic oxidation of alkyl aromatics
-
Oxidation is a major chemical process to produce oxygenated chemicals in both nature and the chemical industry. Presently, the industrial manufacture of benzoic acids and benzene polycarboxylic acids (BPCAs) is mainly based on the deep oxidation of polyalkyl benzene, which is somewhat suffering from environmental and economical disadvantage due to the formation of ozone-depleting MeBr and corrosion hazards of production equipment. In this report, photo-induced deep aerobic oxidation of (poly)alkyl benzene to benzene (poly)carboxylic acids was developed. CeCl3 was proved to be an efficient HAT (hydrogen atom transfer) catalyst in the presence of alcohol as both hydrogen and electron shuttle. Dioxygen (O2) was found as a sole terminal oxidant. In most cases, pure products were easily isolated by simple filtration, implying large-scale implementation advantages. The reaction provides an ideal protocol to produce valuable fine chemicals from naturally abundant petroleum feedstocks. [Figure not available: see fulltext.].
- Wang, Chang-Cheng,Zhang, Guo-Xiang,Zuo, Zhi-Wei,Zeng, Rong,Zhai, Dan-Dan,Liu, Feng,Shi, Zhang-Jie
-
p. 1487 - 1492
(2021/07/10)
-
- Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors
-
CBP bromodomain could recognize acetylated lysine and function as transcription coactivator to regulate transcription and downstream gene expression. Furthermore, CBP has been shown to be related to many human malignancies including acute myeloid leukemia. Herein, we identified DC-CPin734 as a potent CBP bromodomain inhibitor with a TR-FRET IC50 value of 19.5 ± 1.1 nM and over 400-fold of selectivity against BRD4 bromodomains through structure based rational drug design guided iterative chemical modification endeavoring to discover optimal tail-substituted tetrahydroquinolin derivatives. Moreover, DC-CPin734 showed potent inhibitory activity to AML cell line MV4-11 with an IC50 value of 0.55 ± 0.04 μM, and its cellular on-target effects were further evidenced by c-Myc downregulation results. In summary, DC-CPin734 showing good potency, selectivity and anti AML activity could serve as a potent and selective in vitro and in vivo probe of CBP bromodomain and a promising lead compound for future drug development.
- Bi, Xiaoyang,Chen, Yu,Sun, Zhongya,Lu, Wenchao,Xu, Pan,Lu, Tian,Ding, Hong,Zhang, Naixia,Jiang, Hualiang,Chen, Kaixian,Zhou, Bing,Luo, Cheng
-
supporting information
(2020/09/16)
-
- Organic Solvent-Free, Pd(II)-Salan Complex-Catalyzed Synthesis of Biaryls via Suzuki-Miyaura Cross-Coupling in Water and Air
-
With use of a Pd(II)-sulfosalan complex as a water-soluble catalyst, we have developed an efficient synthesis of biaryls via Suzuki-Miyaura cross-coupling in water under aerobic conditions. The water-insoluble target molecules were isolated by simple filtration in analytical purity after washing with 0.01 M aqueous HCl (20 examples). In most cases, palladium contamination was below 5 ppm considered acceptable for active pharmaceutical ingredients. The established method is scalable, reproducible, and provides biaryl products in isolated yields up to 91%.
- Bunda, Szilvia,Udvardy, Antal,Voronova, Krisztina,Joó, Ferenc
-
p. 15486 - 15492
(2019/01/03)
-
- Preparation method of pure water printing paper based on bimetallic complex
-
The invention discloses a preparation method of pure water printing paper. 4-(2-pyridyl)benzaldehyde is used as raw materials; an Ir-Eu bimetallic complex with humidity response characteristics is sequentially obtained through oxidization reaction, metal
- -
-
Paragraph 0038-0041; 0043-0045
(2018/09/08)
-
- A Arylheterocycle chirality bcr - abl inhibitor and its preparation method and application
-
The invention discloses aromatic heterocyclic biphenyl Bcr-Abl inhibitors as well as a preparation method and application thereof. A structural formula of the inhibitors is shown in the specification, wherein in the structural formula, Ar is aromatic heterocycle; R is a mono-substituent or a di-substituent, and the substituent is alkyl or halogen. The series of inhibitors have a certain inhibiting effect on ABL1 kinase in vitro, can inhibit tumor cell proliferation and can be used for preparing antitumor drugs, especially CML (chronic myelocytic leukemia) drugs. The preparation method of the aromatic heterocyclic biphenyl Bcr-Abl inhibitors, which is provided by the invention, has the advantages of easiness in obtainment of raw materials, mild reaction conditions, simplicity in operation of reaction processes and cheap used reagents.
- -
-
Paragraph 0046; 0047; 0048
(2016/10/09)
-
- KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
-
Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
- -
-
Paragraph 0338; 0340; 0522; 0524
(2016/09/26)
-
- Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents
-
As a continuation to our previous research, twenty-eight aromatic-heterocyclic biphenyls were designed and synthesized as novel Bcr-Abl inhibitors. The title compounds were investigated for their antiproliferative activities against wild K562 cells and Imatinib-resistant K562 cells (K562R). The results indicated that most of them exhibited potent Bcr-Abl inhibition and moderate antiproliferative potency against K562 cells. Furthermore, three compounds 3, 7 and 21 displayed moderate antiproliferative activities against K562R cells. Molecular docking indicated that 3 bound more tightly with Bcr-AblT315I compared to Bcr-AblWT. The higher affinity was consistent with its relatively promising K562R cell growth inhibition. These aromatic-heterocyclic biphenyls could be considered as novel lead compound for optimized as Bcr-AblT315I inhibitors. They provide a good starting point for the further development of novel anti-leukemia agents capable of dealing with clinical acquired resistance against Imatinib.
- Dong, Jinyun,Pan, Xiaoyan,Wang, Jinfeng,Su, Ping,Zhang, Lin,Wei, Fen,Zhang, Jie
-
p. 780 - 789
(2015/08/06)
-
- Benzoimidazole derivatives and pharmaceutical composition comprising the same
-
Disclosed herein are novel benzoimidazole derivatives functioning as antagonists to vanilloid receptor-1, and a pharmaceutical composition comprising the same. They are useful in preventing or treating pain, acute pain, chronic pain, neuropathic pain, pos
- -
-
Page/Page column 16; 31-32
(2015/12/17)
-
- Copper-catalysed regioselective azidation of arenes by C-H activation directed by pyridine
-
A novel and efficient copper-catalysed pyridine directed ortho-azidation of arenes has been developed using safe and stable benzotriazole sulphonyl azide as the azidating agent. A variety of organo azides have been synthesized with electron donor and with
- Azad, Chandra S.,Narula, Anudeep K.
-
p. 100223 - 100227
(2015/12/04)
-
- Carboxy derivatised Ir(iii) complexes: synthesis, electrochemistry, photophysical properties and photocatalytic hydrogen generation
-
In this contribution the synthesis and characterisation of a series of novel mixed ligand iridium(iii) complexes, functionalised with a carboxy ester or phosphonate groups are reported. These groupings are introduced on the 4-position of either the phenyl pyridine or the 2,2′-bipyridyl ligands. A low temperature high yield synthesis for the precursor [Ir(ppy-COOEt)2(μ-Cl)]2 was developed. The photophysical and electrochemical properties of these compounds are also described, together with their behaviour as photosensitisers for the generation of hydrogen from water.
- Paul, Avishek,Das, Nivedita,Halpin, Yvonne,Vos, Johannes G.,Pryce, Mary T.
-
p. 10423 - 10430
(2015/06/08)
-
- Phosphorescent biscyclometallated iridium(iii) ethylenediamine complexes functionalised with polar ester or carboxylate groups as bioimaging and visualisation reagents
-
We report the synthesis, characterisation and photophysical properties of new phosphorescent biscyclometallated iridium(iii) ethylenediamine (en) complexes functionalised with polar ester or carboxylate groups [Ir(N^C)2(en)]n(X) (n = +1, X = Cl-, HN^C = methyl 4-(2-pyridyl)benzoate Hppy-COOMe (1a), methyl 2-phenyl-4-quinolinecarboxylate Hpq-COOMe (2a); n = -1, X = Li+, HN^C = 4-(2-pyridyl)benzoate Hppy-COO- (1b), 2-phenyl-4-quinolinecarboxylate Hpq-COO- (2b)). In aqueous solutions, the carboxylate complexes 1b and 2b displayed emission quenching (ca. 7 and 74 fold, respectively) and lifetime shortening upon protonation, and their pKa values were determined to be 5.13 and 3.46, respectively. The pq complexes 2a and 2b exhibited hypsochromic shifts in their emission maxima and a significant increase in emission intensity (ca. 84 and 15 fold, respectively) upon nonspecific binding to the protein bovine serum albumin (BSA). Inductively coupled plasma-mass spectroscopy (ICP-MS) and laser-scanning confocal microscopy (LSCM) results revealed that the ester complexes 1a and 2a were efficiently internalised by the human cervix epithelioid carcinoma (HeLa) cells through energy-requiring pathways and subsequently localised in endosomes and mitochondria, respectively. They showed good biocompatibility in the dark, but became significantly cytotoxic upon photoirradiation due to the generation of singlet oxygen. In contrast, in aqueous solutions of physiological pH, the carboxylate complexes 1b and 2b existed as the anionic form and hardly entered cells due to limited membrane permeability, as evidenced by the intense emission surrounding the plasma membrane of the cells. They showed negligible cytotoxicity and the cell viability remained over 95% for an incubation period of 24 hours. In view of the low cytotoxicity and strongly emissive nature of the hydrophilic ppy-COO- complex 1b in an aqueous medium, the potential application of the complex as a visualisation reagent has been demonstrated using zebrafish (Danio rerio) as an animal model. This journal is
- Tang, Tommy Siu-Ming,Leung, Kam-Keung,Louie, Man-Wai,Liu, Hua-Wei,Cheng, Shuk Han,Lo, Kenneth Kam-Wing
-
p. 4945 - 4956
(2015/03/18)
-
- Dual application of Pd nanoparticles supported on mesoporous silica SBA-15 and MSU-2: Supported catalysts for C-C coupling reactions and cytotoxic agents against human cancer cell lines
-
Two different mesoporous silica-based materials (SBA-15 and MSU-2) have been treated under mild conditions with different quantities of [PdCl2(cod)] (cod = 1,5-cyclooctadiene) to promote the formation of supported palladium nanoparticles (materials of the type SBA-15-Pd and MSU-2-Pd). The synthesized materials have been characterized by different techniques observing that the palladium nanoparticles remain impregnated in the silica. The catalytic activity of the hybrid Pd-silica materials has been tested in Suzuki-Miyaura C-C coupling reactions observing moderate conversion rates in the reactions of 3-bromoanisole with 4-carboxyphenylboronic acid and 2-bromopyridine with 4-carboxyphenylboronic acid. In addition, the synthesized materials showed a good degree of recyclability, being catalytically active in five consecutive catalytic tests. Finally, in order to evaluate the cytotoxicity of the synthesized materials, in vitro tests against five different human cancer cell lines have been carried out, observing high cytotoxic activities of the hybrid systems comparable if not somewhat higher to other systems based on metal complexes supported on mesoporous silicas described previously in the literature. To the best of our knowledge the cytotoxic study reported here represents the first evaluation of the anticancer action of supported palladium nanoparticles in human cancer cells.
- Balbn, Adriana,Gaballo, Francesco,Ceballos-Torres, Jess,Prashar, Sanjiv,Fajardo, Mariano,Kaluderovi, Goran N.,Gmez-Ruiz, Santiago
-
p. 54775 - 54787
(2015/02/02)
-
- Structure-photoluminescence quenching relationships of iridium(III)- tris(phenylpyridine) complexes
-
The synthesis, structural, photophysical, theoretical, and electrochemical characterization of four tris(2-phenylpyridine)-based IrIII complexes are reported. The complexes were functionalized on the pyridine or on the phenyl rings with amide moieties substituted with a tris(ethyl)amine or ethyl groups, thereby yielding a family of compounds with hemicaged or open (without a capping unit but with similar functional groups on the ligand) structure. Within the context of the parent tris(2-phenylpyridine) and the full-cage iridium(III) complexes, structure-photoluminescence quenching relationships (SPQR) of the four complexes have been investigated. Luminescence quenching by oxygen has been studied with Stern-Volmer plots and through evaluation of the thermodynamic parameters involved in the quenching process. Density functional theory (DFT) and time-dependent DFT (TD-DFT) calculations have been performed on the complexes to gain insights into structural and electronicfeatures and the nature of the excited states involved in the electronic absorption processes. Interestingly, shielding by the capping unit of moieties in which the LUMO orbital is mostly localized (on the pyridines) results in a dramatic 40 % decrease in oxygen quenching. Conversely, shielding ofmoieties in which the HOMO orbital is partially localized (on the phenyl rings) does not induce any change in the oxygen quenching degree. In both sets of compounds, the thermodynamic feasibility of oxygen quenching is the same for the hemicaged and open compounds, thus giving evidence of the structural origin of such quenching decrease. The SPQRopens up new routes to the design of tailored, more or less sensitive to oxygen, luminescent iridium complexes (e.g., for use as biolabels). A family of four tris(2-phenylpyridine)-based IrIII complexes with hemicaged or open (without capping unit but with similar functional groups on the ligand) structure are reported. Within the context of the parent tris(2-phenylpyridine) and the full-cage iridium(III) complexes, structure-photoluminescence quenching relationships (SPQR) of the four complexes have been investigated. Copyright
- Ruggi, Albert,Mauro, Matteo,Polo, Federico,Reinhoudt, David N.,De Cola, Luisa,Velders, Aldrik H.
-
scheme or table
p. 1025 - 1037
(2012/05/04)
-
- PYRROLIDINE OR THIAZOLIDINE CARBOXYLIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERSAS AS AGONISTS OF G- PROTEIN COUPLED RECEPTOR 43 (GPR43)
-
The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.
- -
-
Page/Page column 204
(2011/07/07)
-
- Novel yellow phosphorescent iridium complexes containing a carbazole-oxadiazole unit used in polymeric light-emitting diodes
-
Yellow iridium complexes Ir(PPOHC)3 and (PPOHC) 2Ir(acac) (PPOHC: 3-(5-(4-(pyridin-2-yl)phenyl)-1,3,4-oxadiazol-2-yl) -9-hexyl-9H-carbazole) were synthesized and characterized. The Ir(PPOHC) 3 complex has good thermal stability with 5% weight-reduction occurring at 370 °C and a glass-transition temperature of 201 °C. A polymeric light-emitting diode using the Ir(PPOHC)3 complex as a phosphorescent dopant showed a luminance efficiency of 16.4 cd/A and the maximum external quantum efficiency of 6.6% with CIE coordinates of (0.50, 0.49). A white polymeric light-emitting diode was fabricated using Ir(PPOHC)3 which showed a luminance efficiency of 15.3 cd/A, with CIE coordinates of (0.39, 0.44). These results indicate that the iridium complexes containing a linked carbazole-oxadiazole unit are promising candidates in high-efficiency electroluminescent devices.
- Tang, Huaijun,Li, Yanhu,Wei, Caihong,Chen, Bing,Yang, Wei,Wu, Hongbin,Cao, Yong
-
experimental part
p. 413 - 421
(2012/06/18)
-
- BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
-
A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
- -
-
Page/Page column 73
(2009/08/16)
-
- Certain pyrazoline derivatives with kinase inhibitory activity
-
The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.
- -
-
Page/Page column 94-95
(2008/12/06)
-
- Azapeptide derivatives as HIV protease inhibitors
-
This invention relates to novel compounds of the Formula Ib: that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.
- -
-
Page/Page column 20; 35; 37
(2009/01/24)
-
- Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists
-
This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2).
- -
-
Page/Page column 52
(2010/11/25)
-
- MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF
-
The present invention relates to compounds with α7 nAChR agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological, psychiatric, cognitive, immunological and inflammatory disorders.
- -
-
Page/Page column 20
(2010/02/15)
-
- IMIDAZOPYRIDINE DERIVATIVES
-
The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R1 and R2 may be the same or different and stand for C1-6 alkyl or the like, R3 and R4 stand for hydrogen atom, methyl group or the like, W stands for mono- or bi-cyclic 3- to 8-membered aromatic or aliphatic heterocycle or the like, and Ar stands for optionally substituted aromatic heterocycle or the like]. These compounds act as melanin-concentrating hormone receptor antagonist and are useful as medicines for central nervous system disorders, cardiovascular system disorders and metabolic disorders.
- -
-
Page/Page column 29
(2008/06/13)
-
- Amides that inhibit vanilloid receptor subtype 1 (VR1) receptor
-
The present invention relates to compounds of formula (I) that are novel VR1 antagonists useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.
- -
-
Page/Page column 10
(2008/06/13)
-
- NOVEL ETHYLENEDIAMINE DERIVATIVES
-
A compound represented by the following formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q [wherein, R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may have a substituent, or the like; Q2 is a single bond or the like; Q3 represents the following group: -C(R3a)(R4a)-{C(R3b)(R4b)}m1-{C(R3c)(R4c)}m2-{C(R3d)(R4d)}m3-{C(R3e)(R4e)}m4-C(R3f)(R4f)- (in which, R3a to R4e represent hydrogen or the like); T0 represents a carbonyl group or the like; and T1 represents -COCONR- or the like]; or salt thereof, solvate thereof, or N-oxide thereof. The compound is useful as a preventive and/or therapeutic agent for cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
- -
-
Page/Page column 99
(2010/02/14)
-
- Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands
-
Seventeen biarylcarboxybenzamide derivatives were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor (VR1) in rat DRG neurons. The replacement of the piperazine moiety of the lead compound 1 with phenyl ring showed quite enhanced antagonistic activity. Among the prepared derivatives, N-(4-tert-butylphenyl)-4-pyridine-2-yl-benzamide (2, IC 50 = 31 nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2-yl) benzamide (3g, IC50 = 31 nM), showed 5-fold higher antagonistic activity than 1 in 45Ca2+-influx assay.
- Park, Hyeung-Geun,Choi, Ji-Yeon,Kim, Mi-Hyun,Choi, Sea-Hoon,Park, Mi-Kyung,Lee, Jihye,Suh, Young-Ger,Cho, Hawon,Oh, Uhtaek,Kim, Hee-Doo,Joo, Yung Hyup,Shin, Song Seok,Kim, Jin Kwan,Jeong, Yeon Su,Koh, Hyun-Ju,Park, Young-Ho,Jew, Sang-Sup
-
p. 631 - 634
(2007/10/03)
-
- PIPERIDINES USEFUL FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS
-
The invention relates to compounds which are substituted chiral or achiral derivatives of 3- or 4- aminopiperidine of the general formula (I). The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of general formula I and especially their use as inhibitors of β-secretases.
- -
-
-
- ETHYLENEDIAMINE DERIVATIVES
-
The invention relates a compound represented by the formula (1):Q1-Q2-C(=O)-N(R1)-Q3-N(R2)-T1-Q4 wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents -CO- or -SO2-, and a medicine which comprises the compound and is useful for thrombosis and embolism.
- -
-
-
- Preparation of aromatic and heteroaromatic carboxylic acids by catalytic ozonolysis
-
A process for catalytically oxidizing alkylaromatic compounds of the formula (I) Ar—CH2—R where Ar is an optionally substituted, aromatic or heteroaromatic 5-membered or 6-membered ring or a ring system having up to 20 carbon atoms where Ar may optionally be fused to a C1-C6-alkyl group in which up to 2 carbon atoms may be replaced by a heteroatom, and R is hydrogen, phenyl, benzyl or heteroaryl, where the phenyl, benzyl or heteroaryl radicals may also be joined to Ar by a bridge, or R together with Ar forms an optionally substituted ring system which may contain one or more optionally substituted heteroatoms, to the corresponding aromatic or heteroaromatic carboxylic acids in a solvent with ozone in the presence of a transition metal catalyst and optionally in the presence of an acid at a temperature between ?70° C. and 110° C. to the corresponding carboxylic acid.
- -
-
Page/Page column 4
(2008/06/13)
-
- COMPOUNDS AND METHODS
-
This invention relates to substituted heteroanilide compounds which are modulators, agonists or antagonists, of the CCR5 receptior. In addition, this invention relates to the treatment and prevention of disease states mediatd by CCR5.
- -
-
-
- A convenient synthesis of heteroaryl benzoic acids via Suzuki reaction
-
An one step approach to heteroaryl benzoic acids from readily accessible heteroaryl halides and carboxybenzene boronic acids is described. The Suzuki coupling is carried out in the presence of Pd(PPh3)4 and sodium carbonate in aqueous acetonitrile. The scope and limitations of the reaction are discussed.
- Gong, Yong,Pauls, Henry W.
-
p. 829 - 831
(2007/10/03)
-
- Intermediates for the preparation of peptide analogues
-
The invention relates to a novel process for the preparation of compounds of formula I STR1 wherein R1 is hydrogen or a suitable amino-protecting group, R2 is unsubstituted or substituted alkyl, R3 is hydrogen, aryl, heterocyclyl, unsubstituted or substituted alkyl or unsubstituted or substituted cycloalkyl, R4, independently of R1, is hydrogen or a suitable amino-protecting group and m is a number from 1 to 7; and wherein further suitable protecting groups for functional groups may be present; which compounds are antivirally active or can be used as starting materials for pharmaceutically active, especially antiviral compounds. The precursor is an oxo compound, which is in turn prepared by hydrogenation with a suitable complex hydride or with hydrogen in the presence of a suitable catalyst and acyl migration starting from a hydrazone, which is in turn preferably prepared from a nitrile via an imino compound by means of hydrogenation and reaction with a hydrazine derivative, which is prepared from an aldehyde by reaction with a reactive derivative of a carboxylic acid in the presence of a cyanide salt; and the novel intermediates required therefor.
- -
-
-
- Inhibitors of farnesyl-protein transferase
-
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent
- -
-
-
- ANTIVIRALLY ACTIVE HETEROCYCLIC AZAHEXANE DERIVATIVES
-
There are described compounds of formula I*, STR1 wherein R. sub.1 is lower alkoxycarbonyl,R 2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R. sub.3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C 4-C 8 cycloalkyl,R. sub.4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, sulfinyl (--SO--) and sulfonyl (--SO 2--) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl,R 5, independently of R 2, has one of the meanings mentioned for R 2, andR 6, independently of R. sub.1, is lower alkoxycarbonyl,or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS. They exhibit outstanding pharmacodynamic properties.
- -
-
-
