Process for preparing diltiazem

Details Process for preparing diltiazem Process for preparing diltiazem

1996-02-14

1997-07-01

Bond, Robert T.

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

Organic compounds

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

C07D28100, C07D28300, C07D28500

Patent

active

056440545

ABSTRACT:
A process is provided for preparing cis-(+)-hydroxy-5-[2-(dimethylamine)ethyl]-2,3-dihydro-2-(4-methoxyphenyl) -benzothiazepin-4(5H)-one that is a useful intermediate in the preparation of diltiazem. It has been found that the requisite N-alkylation reaction proceeds rapidly and with an excellent yield when the solvent is a mixture of toluene and N-methylpyrrolidin-2-one and the base is finely-divided sodium carbonate under anhydrous conditions. Such diltiazem commonly is used in the treatment of angina pectoris.

REFERENCES:
patent: 3582257 (1971-06-01), Kugita et al.
patent: 4416819 (1983-11-01), Nagao et al.
patent: 4438035 (1984-03-01), Gaino et al.
patent: 4908469 (1990-03-01), Martin
patent: 5514589 (1996-05-01), Kanerva et al.
"Sodium Hydride--DMSO Mixture Explodes", Chem. Eng. News, 44(15), 48 (1966).
Chemical Abstracts, vol. 115, 1991, pp. 969 and 970, Abstract 232305, "Process for Preparing Benzothiazepine Derivatives", Rudolf Kubela et al., Abstract of Canadian Patent No. 1,284,321, granted May 21, 1991.

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