申请人:Ciba-Geigy Corporation
公开号:US05606078A1
公开(公告)日:1997-02-25
Compounds of formula I ##STR1## wherein R.sub.1 is free or esterified carboxy, hydroxymethyl or formyl, R.sub.2 and R.sub.4 are each independently of the other aliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radicals and R.sub.3 is azido, or amino that is aliphatically or araliphatically substituted and/or protected by an amino-protecting group, and the salts thereof, are valuable intermediates in the preparation of medicinal active ingredients, for example of compounds of formula II ##STR2## wherein R.sub.A is an aromatic or heteroaromatic radical, R.sub.2 and R.sub.4 are each independently of the other aliphatic, cycloaliphatic, cycloaliphaticaliphatic or araliphatic radicals, R.sub.3 is unsubstituted or N-mono- or N,N-di-lower alkylated or N-lower alkanoylated amino, and R.sub.B is an aliphatically, cycloaliphatically or heteroaromatically-aliphatically substituted amino group, and the salts thereof, which can be used, for example, as antihypertensives.
式子I的化合物 ##STR1## 其中R.sub.1是自由的或酯化的羧基,羟甲基或甲酰基,R.sub.2和R.sub.4分别是独立的脂肪族,环脂肪族-脂肪族,芳基脂肪族或杂环芳基脂肪族基团,R.sub.3是偶氮基或氨基,该氨基是经过脂肪族或芳基脂肪族取代和/或由氨基保护基保护的,以及它们的盐,在制备药物活性成分,例如式子II的化合物 ##STR2## 中是有价值的中间体,其中R.sub.A是芳香或杂芳基基团,R.sub.2和R.sub.4分别是独立的脂肪族,环脂肪族,环脂肪族-脂肪族或芳基脂肪族基团,R.sub.3是未取代的或N-单或N,N-二-较低烷基化或N-较低烷酰化的氨基,R.sub.B是脂肪基,环脂肪基或杂芳基-脂肪基取代的氨基,以及它们的盐,可以用作例如降压剂。