摘要 |
A process of preparing perindopril of formula (I), or a pharmaceutically acceptable salt thereof which process comprises protecting a compound of formula (II) where R denotes a hydrogen atom, in the presence of benzene sulphonic acid as a catalyst, to obtain the benzene sulphonic acid salt of an ester of formula (III) where Rl is a carboxyl protecting group and reacting said ester of formula (III) with N-[(S)-1-carbethoxybutyl]-(S)-alanine to obtain a compound of formula (IV) where Rl is as defined above; and deprotecting a compound of formula (IV) to yield perindopril of formula (I), or a pharmaceutically acceptable salt thereof. There is also provided by the present invention the benzene sulphonic acid salt of an ester of formula (III), and perindopril or a pharmaceutically acceptable salt thereof prepared by the above process. |
申请人 |
CIPLA LIMITED;KANKAN, RAJENDRA, NARAYANRAO;RAO, DHARMARAJ, RAMACHANDRA;WAIN, CHRISTOPHER, PAUL |
发明人 |
KANKAN, RAJENDRA, NARAYANRAO;RAO, DHARMARAJ, RAMACHANDRA |