2β-(4′-甲基- 1′-哌嗪基)- 3α-羟基-16,17-取代-5α-雄甾烷的合成

SYNTHESIS OF 2β-(4’-METHYL-1’-PIPERAZINO)-3α-HYDROXYL-16,17-SUBSTITUTED-5α-ANDROSTANES

为了寻找心血管系统药物,以表雄酮为原料,合成了7个16,17位取代的目标化合物:2β-(4’-甲基-1’-哌嗪基)-3α-羟基-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α-羟基-16α-溴-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-氧-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-肟-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17β-氨基-5α-雄甾烷和2β—(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-16β-氨基-5α-雄甾烷。初步药理试验结果表明它们都有不同程度的抗心律失常活性。

According to some studies, the vicinal amino-alcohol compounds of5α- androstane possess to a certain extent biological activities in cardiovascular system. Inorder to find new antiarrhythmic agents, seven new 2β- ( 4'- methyl- 1'- piperazino)-3α- hydroxyl- 16, 17- substituted- 5α - adrostanes were synthesized through 2α,3α- epoxyl- 5α - adrostan- 17- one from epiandrosterone. Preliminary results of biologicalexperiment showed that they possess to a different extent antiarrhythmic activities amongwhich compounds VI, XI and XIV showed higher activities than others.