Invention Grant
- Patent Title: Process for the preparation of carvedilol
- Patent Title (中): 卡维地洛的制备方法
-
Application No.: US11568785Application Date: 2005-05-19
-
Publication No.: US07705163B2Publication Date: 2010-04-27
- Inventor: Rajendra Narayanrao Kankan , Dharmaraj Ramachandra Rao
- Applicant: Rajendra Narayanrao Kankan , Dharmaraj Ramachandra Rao
- Applicant Address: IN Mumbai
- Assignee: Cipla Limited
- Current Assignee: Cipla Limited
- Current Assignee Address: IN Mumbai
- Agency: Conley Rose, P.C.
- Agent Rodney B. Carroll
- Priority: GB0411273.6 20040520
- International Application: PCT/GB2005/001978 WO 20050519
- International Announcement: WO2005/113502 WO 20051201
- Main IPC: C07D209/82
- IPC: C07D209/82

Abstract:
A process for the preparation of carvedilol of formula (I) (I) either in enantiomeric substantially pure form, or as an enantiomeric mixture, optionally as a pharmaceutically acceptable salt thereof, which process comprises reacting 2,3-eopxypropoxy carbazole of formula (II) (II) or the R or S enantiomer thereof, with N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) (V) to yield benzyl carvedilol of formula (VI) (VI) which is debenzylated by catalytic hydrogenation to yield carvedilol of formula (I), either in enantiomeric substantially pure form, or as an enantiomeric mixture, and if desired reacting the thus formed carvedilol of formula (I) with an inorganic or organic acid to yield a pharmaceutically acceptable salt thereof, and/or, if desired, separating the enantiomers. The above process is characterised in that reaction of said 2,3-epoxypropoxy carbazole of formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) is carried out in water as the reaction medium. The present invention further provides carvedilol of formula (I) prepared by a process as described above, and pharmaceutical compositions containing the same and therapeutic uses thereof.
Public/Granted literature
- US20080234492A1 Process for the Preparation of Carvedilol Public/Granted day:2008-09-25
Information query