A phenylalkylaminoethylsalicylamide, its preparation and pharmaceutical compositions containing it
申请人:SCHERING CORPORATION
公开号:EP0009702A1
公开(公告)日:1980-04-16
The (R,R) optical isomer of labetalol, namely 5-[ (R)-1-hydroxy- 2-[(R)-1-methyl- 3-phenylpropyl)amino ]ethyl] salicylamide, and its pharmaceutically acceptable acid addition salts, in a state substantially free of the corresponding (R,S), (S,R) and (S,S) optical isomers, are novel compounds with favourable therapeutic properties in comparison with labetalol. They can be used in particular in the treatment of hypertension.
The novel (R,R) optical isomer and its pharmaceutically acceptable acid addition salts can be prepared by removal of the protecting groups from an N,O-protected (R,R) optical isomer or acid addition salt thereof, wherein the basic nitrogen atom and the phenolic hydroxy group are protected, preferably by hydrogenolytic removal of hydrogenolysable groups.
拉贝洛尔的(R,R)光学异构体,即5-[(R)-1-羟基-2-[(R)-1-甲基-3-苯丙基)氨基]乙基]水杨酰胺,及其药学上可接受的酸加成盐,在基本上不含相应的(R,S)、(S,R)和(S,S)光学异构体的状态下,是一种新型化合物,与拉贝洛尔相比,具有良好的治疗特性。它们尤其可用于治疗高血压。
新型(R,R)光学异构体及其药学上可接受的酸加成盐可以通过去除N,O保护的(R,R)光学异构体或其酸加成盐中的保护基团来制备,其中碱性氮原子和酚羟基受到保护,最好通过氢解去除可氢解基团。