申请人:Merck & Co., Inc.
公开号:US04628084A1
公开(公告)日:1986-12-09
The present invention provides an improved process for producing 3-acylamino benzodiazepines of the formula: ##STR1## wherein: R is loweralkyl of from 1-6 carbon atoms, aryl such as phenyl and halophenyl, aralkyl, alkyloxy, aralkyloxy, indolyl or substituted indolyl; R' is hydrogen, loweralkyl of from 1-6 carbon atoms, carboxymethyl or carbalkoxymethyl wherein the alkoxy groups contain from 1-4 carbon atoms; X is hydrogen or halogen; Y is hydrogen or halogen. These compounds are useful because of their activity as cholecystokinin (CCK) inhibitors.
本发明提供了一种改进的方法,用于生产公式为:##STR1## 的3-酰胺基苯二氮平衍生物,其中:R是1-6个碳原子的低碳基,如苯基和卤苯基,芳基烷基,烷氧基,芳基烷氧基,吲哚基或取代吲哚基;R'是氢,1-6个碳原子的低碳基,羧甲基或卡巴洛甲氧基,其中烷氧基含有1-4个碳原子;X是氢或卤素;Y是氢或卤素。这些化合物因其作为胆囊收缩素(CCK)抑制剂的活性而有用。