PREPARATION OF 1,5-BENZOTHIAZEPINE DERIVATIVES BY REACTING 2-PHENYL-3-HYDROXY N-UNSUBSTITUTED BENZOTHIZEPINONE WITH N,N-DIALKYL AMINO ETHA

摘要

PURPOSE:To readily obtain the titled compound useful as a drug, having hypotensive action, vasodilating action on cerebral blood vessel and crown blood vessel, by condensing an N-nonsubstituted 1,5-benzothiqazepine derivative as a raw material with an aminoethanol derivative. CONSTITUTION:An N-nonsubstituted 1,5-benzothiazepine derivative shown by formula I (R1 is lower alkyl or lower alkoxy; R2 is H or lower alkanoyl; one of R3 and R4 is lower alkyl or halogen atom. and the other H) is used as a raw material and condensed with an aminoethanol derivative shown by formula II (R5 and R6 are lower alkyl; Z is H, lower alkylsulfonyl, arylsulfonyl or sulfo). In the reaction, when Z of the compound shown by formula II is preferably H, the reaction is carried out in the presence of a dehydrating agent and when Z is lower alkylsulfonyl, the reaction is done is the presence of an alkali reagent to give a compound shown by formula III.