Sulfonamide peri-substituted bicyclics for occlusive artery disease
申请人:Singh Jasbir
公开号:US20060079520A1
公开(公告)日:2006-04-13
Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula
A representative example is:
CARBOXYLIC ACID PERI - SUBSTITUTED BICYCLICS FOR OCCLUSIVE ARTERY DISEASE
申请人:Decode Genetics, Inc.
公开号:EP1814881A2
公开(公告)日:2007-08-08
[EN] CARBOXYLIC ACID PERI - SUBSTITUTED BICYCLICS FOR OCCLUSIVE ARTERY DISEASE<br/>[FR] BICYCLIQUES PERI-SUBSTITUES D'ACIDES CARBOXYLIQUES UTILISES LORS D'UNE MALADIE ARTERIELLE OCCLUSIVE
申请人:DECODE CHEMISTRY INC
公开号:WO2006044415A2
公开(公告)日:2006-04-27
[EN] Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. [FR] L'invention concerne des acides carboxyliques à noyau bicyclique fusionné péri-substitué, destinés au traitement ou à la prévention d'une maladie ou d'un état à médiation par prostaglandines.
Regiospecific synthesis of 3-alkyl-4-hydroxybenzimidazoles as intermediates for an expedient approach to potent EP3 receptor antagonists
作者:Wayne Zeller、Alex S. Kiselyov、Jasbir Singh
DOI:10.1016/j.tetlet.2010.01.005
日期:2010.3
Regiospecific construction of 3-alkyl-4-hydroxybenzimidazoles is detailed. The synthetic route involves a novel O- to N-acyl transfer reaction to address the observed exclusive O-acylation of 2-amino-3-nitrophenol starting material. This efficient route provides the targeted 3-alkyl-4-hydroxybenzimidazoles in good yields, in five steps, without the use of chromatographic purification. These key intermediates were subsequently elaborated, as shown, to provide acylsulfonamide-derived potent EP3 receptor antagonists. (C) 2010 Elsevier Ltd. All rights reserved.