NEW PROCESS FOR THE SYNTHESIS OF IMIDAZO[4,5-B]PYRIDINE DERIVATIVES AS POTENT ORALLY-ACTIVE THROMBOXANE-A2 RECEPTOR ANTAGONISTS

被引：10
|
作者：
NICOLAI, E
CLAUDE, S
TEULON, JM
机构：
[1] Carpibem, Rueil Malmaison, 92500
来源：
JOURNAL OF HETEROCYCLIC CHEMISTRY | 1994年 / 31卷 / 01期
关键词：
D O I：
10.1002/jhet.5570310113
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A new synthetic route to prepare the 4-[3-(4-chlorophenyl)methyl-6-chloroimidazo[4,5-b]pyridin-2-yl]-3,3-dimethylbutanoic acid (UP 116-77) is described. UP 116-77 is a potent orally active TXA2/PGH2 receptor antagonist currently under pharmacological investigation. Its development needed a suitable synthesis for industrial processing. The cyclization of 3-amino-5-chloro-2-(4-chlorophenyl)methylaminopyridine 4 with 3,3-dimethylglutaric anhydride in refluxing acetic acid affords a new efficient and simple way to UP 116-77 and subsequently to various 2-substituted imidazo[4,5-b]pyridine derivatives.
引用
收藏
页码：73 / 75
页数：3
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