PURPOSE: To prepare the titled compound useful as a remedy for stenocardia such as angia of effort, inveterate myocardial infarction, etc., in high yield, by reacting a 3-hydroxy derivative with dimethylaminoethyl halide, and successively acetylating, debenzylating and alkylating the product.
CONSTITUTION: 2-( 4-Benzyloxyphenyl )-3-hydroxy-2,3-dihydro-1,5-benzothiazepin- 4(5H)-one of formula II is made to react with dimethylaminoethyl halide to obtain a novel compound of formula III, which is acetylated with acetyl anhydride, acetyl halide, etc. The resultant novel compound of formula IV is debenzylated with acetic acid solution of hydrogen bromide, etc. to obtain a novel compound of formula V, which is converted to the objective compound of formula Iby the alkylation in the presence of a basic reagent such as lithium hydride, sodium hydroxide, etc. In the reaction formula, X represents halogen, and R represents alkyl.
UNEDA TAKASHI
SASAO YASUTAKA
TAKATANI MASAHIRO
| JP46016988A | ||||
| JP46043785A | ||||
| JP46016749A |