Azidolysis of epoxides catalysed by the halohydrin dehalogenase from Arthrobacter sp. AD2 and a mutant with enhanced enantioselectivity: an (S)-selective HHDH
摘要:
Halohydrin dehalogenase from Arthrobacter sp. AD2 catalysed azidolysis of epoxides with high regioselectivity and low to moderate (S)-enantioselectivity (E = 1-16). Mutation of the asparagine 178 to alanine (N178A) showed increased enantioselectivity towards styrene oxide derivatives and glycidyl ethers. Conversion of aromatic epoxides was catalysed by HheA-N178A with complete enantioselectivity, however the regioselectivity was reduced. As a result of the enzyme-catalysed reaction, enantiomerically pure (S)-beta-azido alcohols and (R)-alpha-azido alcohols (ee >= 99%) were obtained. (C) 2016 Published by Elsevier Ltd.
[EN] HETEROARYL-ETHANOLAMINE DERIVATIVES AS ANTIVIRAL AGENTS<br/>[FR] DERIVES D'HETEROARYL-ETHANOLAMINE EN TANT QU'AGENTS ANTIVIRAUX
申请人:UPJOHN CO
公开号:WO2004022567A1
公开(公告)日:2004-03-18
The present invention provides a compound of formula (I), which are useful as antiviral agents, in particular, as agents against viruses of the herpes family.
本发明提供了一种化合物(I)的公式,其作为抗病毒剂特别是抗疱疹病毒家族的药剂。
NOVEL PROCESS TO PREPARE PIOGLITAZONE VIA SEVERAL NOVEL INTERMEDIATES
申请人:Pandey Bipin
公开号:US20140088127A1
公开(公告)日:2014-03-27
A novel process for preparing thiazolidinediones, preferably Pioglitazone, as described. Also described are novel intermediates involved in its synthesis and process for their preparation and use in medicine.
Novel process to prepare pioglitazone via several novel intermediates
申请人:Pandey Bipin
公开号:US20080300282A1
公开(公告)日:2008-12-04
A novel process for preparing thiazolidinediones, preferably Pioglitazone, as described. Also described are novel intermediates involved in its synthesis and process for their preparation and use in medicine.
Imidazo[2,1-b]thiazoles carrying in the 2-position a phenyl radical unsubstituted or substituted by one or two atoms or radicals selected from halogen atoms and alkyl, alkoxy, alkylthio, dialkylamino, dialkylsulphamoyl, nitro, cyano and trifluoromethyl radicals or carrying in the 2-position a 2-, 3- or 4-pyridyl radical unsubstituted or substituted by an alkyl or alkoxy radical, are new compounds possessing pharmacological properties and useful, in particular, as anti-depressants and psycho-energisers.
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases
作者:Mark E. Schnute、David J. Anderson、Roger J. Brideau、Fred L. Ciske、Sarah A. Collier、Michele M. Cudahy、MariJean Eggen、Michael J. Genin、Todd A. Hopkins、Thomas M. Judge、Euibong J. Kim、Mary L. Knechtel、Sajiv K. Nair、James A. Nieman、Nancee L. Oien、Allen Scott、Steven P. Tanis、Valerie A. Vaillancourt、Michael W. Wathen、Janet L. Wieber
DOI:10.1016/j.bmcl.2007.03.102
日期:2007.6
A novel series of 2-aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridine-5-carboxamides have been identified as potent antivirals against human herpesviruses. These compounds demonstrate broad-spectrum inhibition of the herpesvirus polymerases HCMV, HSV-1, EBV, and VZV with high specificity compared to human DNA polymerases. (c) 2007 Elsevier Ltd. All rights reserved.