Process for the preparation of a benzothiazepine

Details Process for the preparation of a benzothiazepine Process for the preparation of a benzothiazepine

1997-03-21

1999-01-12

Berch, Mark L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

C07D28110

Patent

active

058592415

ABSTRACT:
Process for the preparation of a 1,5-benzothiazepine derivative, or a salt thereof, of formula 1 ##STR1## where R1 represents H, an alkyl group or an alkoxy group and R.sub.2 represents H or a halogen, in which process a propanoic acid derivative of formula 2 ##STR2## where R.sub.1 and R.sub.2 are as defined above and R.sub.3 represents H or an alkyl group is subjected to an intramolecular cyclisation reaction in a non-halogenated solvent in the presence of a carboxylic acid. Preferably, R.sub.2 is H and R.sub.1 is OCH.sub.3. Trichloroacetic acid is preferably used as .alpha.-chlorinated acid. The benzothiazepine obtained on cyclisation can be subjected to an alkylation reaction and/or an acylation reaction to obtain known pharmaceutical products, in particular diltiazem.

REFERENCES:
patent: Re34935 (1995-05-01), Rossey
patent: 3562257 (1971-02-01), Kugita et al.
patent: 5013835 (1991-05-01), Rossey
patent: 5102998 (1992-04-01), Rossey
patent: 5128469 (1992-07-01), Nishimoto
patent: 5294706 (1994-03-01), Koumoto

Affiliated with

Also associated with

Rating

Process for the preparation of a benzothiazepine does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Process for the preparation of a benzothiazepine, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process for the preparation of a benzothiazepine will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1517892