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
Authors
Dates
1999-11-27—Published
1995-09-15—Filed