METHOD OF SYNTHESIS OF 3-HYDROXY-5-[2-(DIMETHYLAMINO)-ETHYL]- -2,3-DIHYDRO-4-(METHOXYPHENYL)-1,5-BENZOTHIAZEPINE-4-(5H)-ON'E METHOD OF SYNTHESIS OF BENZOTHIAZEPINE DERIVATIVES, METHOD OF SYNTHESIS OF CIS-(+)-3-ACETOXY-5-[2-(DIMETHYLAMINO)-ETHYL]- -2,3-DIHYDRO-2-(4-METHOXYPHENYL)-1,5-BENZOTHIAZEPINE-4-(5H)-ON'E Russian patent published in 1999 - IPC

Abstract RU 2141957 C1

FIELD: organic chemistry, chemical technology. SUBSTANCE: invention relates to a method of synthesis of 3-hydroxy-5- -[2-(dimethylamino)-ethyl]-2,3-dihydro-4-(methoxyphenyl)-1,5- -benzothiazepine-4-(5H)-on'e of the general formula (I) and its salts that can be used for synthesis of pharmaceutically active compounds, for example, diltiazem that is used in cardiovascular therapy. Method involves the reaction of N-alkylation of 3-hydroxy-2,3-dihydro-4-(methoxyphenyl)-1,5- -benzothiazepine-4-(5H)-on'e of the formula (II) with (dimethylamino)-ethyl halide and this reaction of N-alkylation is carried out in the reaction mixture containing 2-butanol and water. EFFECT: simplified method, increased effectiveness and safety as compared with the known ones, high purity of the end product. 11 cl, 2 ex

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RU 2 141 957 C1

Authors

Martti Khjutenen

Dates

1999-11-27Published

1995-09-15Filed