Process for preparing a pharmaceutically active compound...

Details Process for preparing a pharmaceutically active compound... Process for preparing a pharmaceutically active compound...

2006-07-04

2006-07-04

Saeed, Kamal A. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S126000

Reexamination Certificate

active

07071209

ABSTRACT:
The invention relates to a process for preparing granisetron, or a pharmaceutically acceptable salt thereof, which comprises: a) cyclisation of a compound of formula (I) in an inert solvent and at a temperature between 0–100° C., in the presence of a strong acid, in order to yield the compound of formula (II); b) methylation of the compound of formula (II), with an alkylating agent, in the presence of a base, in an inert solvent and at a temperature between 0° C.–160° C., and with optional formation of a pharmaceutically acceptable salt. The process of the invention yields a granisetron of high purity, preventing impurities due to demethylation, by carrying out the methylation after rather than before cyclisation and with a higher yield.

REFERENCES:
patent: 0200444 (1986-11-01), None
patent: 2129349 (1997-02-01), None
patent: 9523799 (1995-09-01), None
patent: 9730049 (1997-08-01), None

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