A process for the preparation of diltiazem

C - Chemistry – Metallurgy – 07 – D

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C07D 281/02 (2006.01) C07D 281/10 (2006.01)

Patent

CA 2098114

(+)-Cis-3-(acetoxy)-5-[2-(dimethylamino)-ethyl]-2,3-dihydro-2-(4- methoxyphenyl)-1,5-benzothiazepin-4(5H)-one hydroch- loride is prepared by N-alkylation of (+)-cis-3-hydroxy-2,3-dihydro-2-(4- methoxyphenyl)-1,5-benzothiazepin-4(5H)-one with di- methylaminoethyl chloride and- K2CO3 in toluene/water, addition of a solubilizing agent and in the presence of a phase- transfer catalyst, the toluene phase being directly subjected to the final O- acetylation.

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