cas 69604-00-8, ETHYL 5-NITROBENZOFURAN-2-CARBOXYLATE

Articles about 69604-00-8Total 15 be found

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[...] intermediate synthetic method (by machine translation)
The invention relates to a [...] intermediate synthesis method, in order to 6 - nitro coumarin as the starting the raw materials, through ring-opening, the ring in the molecule, esterification, reduction, paipai qin link other steps, to obtain key [...] middle style I compound 5 - (1 - piperazinyl) - 2 - benzofuran - 2 - carboxylic acid ethyl ester. The invention synthetic route is simple, the target product yield is relatively high, and is suitable for industrial scale production. (by machine translation)
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(2018/04/01)

Synthetic method for vilazodone intermediate ethyl 5-(1-piperazinyl)-2-benzofuran-2-carboxylate
The invention relates to a synthetic method for a vilazodone intermediate, i.e., ethyl 5-(1-piperazinyl)-2-benzofuran-2-carboxylate. The key vilazodone intermediate ethyl 5-(1-piperazinyl)-2-benzofuran-2-carboxylate as shown in a formula I is prepared with 6-nitrocoumarin as a starting raw material through addition, ring opening, intramolecular ring closure, nitro reduction, piperazine ring preparation, etc. The synthetic method is simple in synthetic route, high in the yield of target products and suitable for industrial scale-up production.
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Paragraph 0032-0034

(2018/03/01)

Pyrimidine heterocyclic compounds, pyrimidine heterocyclic compound salts, and preparation method and application thereof
The invention provides pyrimidine heterocyclic compounds, pyrimidine heterocyclic compound salts, and a preparation method and application thereof. According to the pyrimidine heterocyclic compounds provided by the invention, specific Rq is selected, so that the obtained compounds have favorable drug resistance and long half life when being used as the medicine for treating or preventing HIV. The compounds have the advantages of high activity, low toxicity and high stability.
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Paragraph 0147; 0148; 0149; 0150

(2017/07/26)

PROCESS FOR THE PREPARATION OF VILAZODONE HYDROCHLORIDE AND ITS AMORPHOUS FORM
The present invention relates to an improved process for the preparation of vilazodone Hydrochloride and a process for preparation of novel pure amorphous form of vilazodone hydrochloride.
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Paragraph 0124

(2015/03/31)

An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition
A series of twenty eight molecules of ethyl 5-(piperazin-1-yl)benzofuran-2-carboxylate and 3-(piperazin-1-yl)benzo[d]isothiazole were designed by molecular hybridization of thiazole aminopiperidine core and carbamide side chain in eight steps and were screened for their in vitro Mycobacterium smegmatis (MS) GyrB ATPase assay, Mycobacterium tuberculosis (MTB) DNA gyrase super coiling assay, antitubercular activity, cytotoxicity and protein-inhibitor interaction assay through differential scanning fluorimetry. Also the orientation and the ligand-protein interactions of the top hit molecules with MS DNA gyrase B subunit active site were investigated applying extra precision mode (XP) of Glide. Among the compounds studied, 4-(benzo[d]isothiazol-3-yl)-N-(4-chlorophenyl)piperazine-1-carboxamide (26) was found to be the most promising inhibitor with an MS GyrB IC50 of 1.77 ± 0.23 μM, 0.42 ± 0.23 against MTB DNA gyrase, MTB MIC of 3.64 μM, and was not cytotoxic in eukaryotic cells at 100 μM. Moreover the interaction of protein-ligand complex was stable and showed a positive shift of 3.5 °C in differential scanning fluorimetric evaluations.
Reddy, Kummetha Indrasena,Srihari, Konduri,Renuka, Janupally,Sree, Komanduri Shruthi,Chuppala, Aruna,Jeankumar, Variam Ullas,Sridevi, Jonnalagadda Padma,Babu, Kondra Sudhakar,Yogeeswari, Perumal,Sriram, Dharmarajan
p. 6552 - 6563
(2015/02/18)

Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis
DNA gyrase of Mycobacterium tuberculosis (MTB) is a type II topoisomerase and is a well-established and validated target for the development of novel therapeutics. By adapting the medium throughput screening approach, we present the discovery and optimization of ethyl 5-(piperazin-1-yl) benzofuran-2- carboxylate series of mycobacterial DNA gyraseB inhibitors, selected from Birla Institute of Technology and Science (BITS) database chemical library of about 3000 molecules. These compounds were tested for their biological activity; the compound 22 emerged as the most active potent lead with an IC50 of 3.2 ± 0.15 μM against Mycobacterium smegmatis DNA gyraseB enzyme and 0.81 ± 0.24 μM in MTB supercoiling activity. Subsequently, the binding of the most active compound to the DNA gyraseB enzyme and its thermal stability was further characterized using differential scanning fluorimetry method.
Renuka, Janupally,Reddy, Kummetha Indrasena,Srihari, Konduri,Jeankumar, Variam Ullas,Shravan, Morla,Sridevi, Jonnalagadda Padma,Yogeeswari, Perumal,Babu, Kondra Sudhakar,Sriram, Dharmarajan
p. 4924 - 4934
(2014/10/16)

Facile microwave-assisted synthesis of substituted benzofuran derivatives
A series of benzofuran derivatives have been synthesized by use of a microwave-assisted process. Substituted or unsubstituted ?- hydroxyacetophenone and salicylaldehyde reacted with ethyl bromoacetate, ω-bromoacetophenone, or chloroacetone under the action of potassium carbonate in DMF to yield substituted benzofuran derivatives. Compared with conventional heating, this microwave-assisted synthetic process has the advantages of more convenient operation, shorter reaction time, and higher yield.
Liu, Junqiang,Mi, Chenggen,Tang, Xuemei,Cao, Yuan,Li, Zicheng,Huang, Wencai
p. 2083 - 2090
(2014/05/06)

PROCESS FOR THE PREPARATION OF VILAZODONE HYDROCHLORIDE AND ITS AMORPHOUS FORM
The present invention relates to an improved process for the preparation of vilazodone Hydrochloride and a process for preparation of novel pure amorphous form of vilazodone hydrochloride.
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Page/Page column 23

(2013/11/05)

Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2- phenylethyl)arylamides
A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3-72 μM compared with the standard ketoconazole IC50 0.52 μM, with the styryl derivative (11c) displaying enhanced activity (IC50 = 0.3 μM) compared with the standard, providing a useful preliminary lead for drug development.
Aboraia, Ahmed S.,Yee, Sook Wah,Gomaa, Mohamed Sayed,Shah, Nikhil,Robotham, Anna C.,Makowski, Bart,Prosser, David,Brancale, Andrea,Jones, Glenville,Simons, Claire
experimental part
p. 4939 - 4946
(2010/09/10)

EP2 RECEPTOR AGONISTS
A compound of Formula (I) or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of Formulae (Ai), (Aii), (Aiii) D is selected from Formulae (Di), (Dii), (Diii), (Div), (Dv) B is selected from the group consisting of Formulae (Bi), (Bii), (Biii), (Biv) (Bv).
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Page/Page column 145

(2008/06/13)

Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
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(2008/06/13)

Vitronectin receptor antagonists
Compounds of formula (I) are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis.
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(2008/06/13)

Probes for imidazoline binding sites: Synthesis and evaluation of a selective, irreversible I2 ligand
An irreversible ligand (7) has been prepared based on the selective I2 ligand 2-BFI. Compound 7 displayed high affinity and selectivity for I2-sites and has been shown to irreversibly bind to these sites in rat brain. Compound 7 should, therefore, prove an invaluable tool for the further elucidation of I2-site function. (C) 2000 Elsevier Science Ltd. All rights reserved.
Coates, Philippa A.,Grundt, Peter,Robinson, Emma S.J.,Nutt, David J.,Tyacke, Robin,Hudson, Alan L.,Lewis, John W.,Husbands, Stephen M.
p. 605 - 607
(2007/10/03)

Vitronectin receptor antagonists
PCT No. PCT/US96/20327 Sec. 371 Date Jul. 27, 1999 Sec. 102(e) Date Jul. 27, 1999 PCT Filed Dec. 20, 1996 PCT Pub. No. WO97/24124 PCT Pub. Date Jul. 10, 1999Compounds of formula (I) are disclosed, wherein: A is a fibrinogen antagonist template; W is a linking moiety of the form -(CHRg)a-U-(CHRg)b-V-; Q1, Q2, Q3 and Q4 are independently N or C-Ry, provided that no more than one Q1, Q2, Q3 and Q4 is N; R' is H or C1-6alkyl, C3-7cycloalkyl-C0-6-alkyl or Ar-C0-6alkyl; Rg is H or C1-6alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl or Ar-C0-6alkyl; Rk is Rg, -C(O)Rg or -C(O)ORg Ri is H, C1-6alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl-U'-C1-6alkyl, C3-7cycloalkyl-C0-6alkyl-U'-C1-6alkyl or Ar-C0-6alkyl-U'-C1-6alkyl; Ry is H, halo, -ORg, -SRg, -CN, -NRgRk, -NO2, -CF3, CF3S(O)r, -CO2Rg, -CORg or -CONRg2, or C1-6alkyl optionally substituted by halo, -ORg, -SRg, -CN, -NR8R'', -NO2, -CF3, R'S(O)3-, -CO2Rg, -CORg or -CONRg2; U and V are absent or CO, CRg2, C(=CRg2), S(O)c, O, NRg, CRgORg, CRg(ORk)CRg2, CRg7CRg(ORk), C(O)CRg2, CRg2C(O), CONRi, NRiCO, OC(O), C(O)O, OC(S), C(S)NRg, NR8C(S), S(O2NRg, NRgS(O)2N=N, NRgNRg, NRgCRg2, NRgCRg2, CRg2O, OCRg2, CRg=CRg, C=C, Ar or Het; a is 0, 1 or 2; c is 0, 1 or 2; r is 0, 1 or 2; and u is 0 or 1; or pharmaceutically acceptable salts thereof, which are vitronectin receptor antagonists useful in the treatment of osteoporosis.
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(2008/06/13)

Benzofuran Derivatives. II. Synthesis of 2,3-Dihydrobenzofurans from Ethyl 2-Acylphenoxyacetates
Ethyl 3-alkyl-3-hydroxy-5-nitro-2,3-dihydro-2-benzofurancarboxylates were obtained from the reaction of ethyl 2-acyl-4-nitrophenoxyacetates with potassium hydroxide in dry dioxane.The relative ratios of the cis and trans isomers with respect to C-2 and C-3 stereochemistry varied according to the structure of the acyl group.When the acyl group was acetyl, propionyl, or isobutyryl group, the cis isomers (2-alkoxycarbonyl groups and 3-hydroxyl groups are cis) were exclusively obtained in high yields.On the other hand, a nearly equimolecular amount of the cis and trans isomers was obtained from the reaction of 2-formyl derivatives under the same conditions.
Suzuki, Tsuneo
p. 2821 - 2825
(2007/10/02)

Chemical Properties

Appearance/Colour :Light yellow to light brown powder
Melting Point: 150 °C
Boiling Point: 359.7 °C at 760 mmHg
Flash Point:171.3 °C
Density: 1.362 g/cm³
Solubility:slightly sol. in Acetone
Storage Temp.:Sealed in dry,Room Temperature
Vapor Pressure: 2.34E-05mmHg at 25°C
Refractive Index: 1.603
PSA: 85.26000
LogP: 3.04090

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69604-00-8

Articles about 69604-00-8Total 15 be found

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Chemical Properties

Appearance/Colour :Light yellow to light brown powder

Melting Point: 150 °C

Boiling Point: 359.7 °C at 760 mmHg

Flash Point:171.3 °C

Density: 1.362 g/cm³

Solubility:slightly sol. in Acetone

Storage Temp.:Sealed in dry,Room Temperature

Vapor Pressure: 2.34E-05mmHg at 25°C

Refractive Index: 1.603

PSA: 85.26000

LogP: 3.04090

Global suppliers and manufacturers of 69604-00-8total 106 suppliers on LookChem

Article Database

69604-00-8

Articles about 69604-00-8Total 15 be found

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Chemical Properties

Appearance/Colour :Light yellow to light brown powder

Melting Point: 150 °C

Boiling Point: 359.7 °C at 760 mmHg

Flash Point:171.3 °C

Density: 1.362 g/cm3

Solubility:slightly sol. in Acetone

Storage Temp.:Sealed in dry,Room Temperature

Vapor Pressure: 2.34E-05mmHg at 25°C

Refractive Index: 1.603

PSA: 85.26000

LogP: 3.04090

Global suppliers and manufacturers of 69604-00-8total 106 suppliers on LookChem

Density: 1.362 g/cm³