PROCEDIMIENTO PARA LA PREPARACION DE NUEVOS DERIVADOS DE TIAZEPINA.

摘要

1,211,171. Thieno-benzothiazepines. J. R. GEIGY A.G. 29 Nov., 1968 [30 Nov., 1967; 29 Dec., 1967], No. 56702/68. Heading C2C. Novel thieno-benzothiazepines of Formula (I) in which n is 2 or 3, R is hydrogen or methyl, X is hydrogen or chlorine and Z is hydrogen, C 1-4 alkyl, C 1-4 hydroxyalkyl, C 3-9 alkanoyloxyalkyl or cyclopropyl, and their acid addition salts, are prepared by reacting a compound of Formula (II) in which Q is halogen or C 1-4 alkoxy, with a compound of Formula (III) in which Z has the same meaning as Z or it represents a radical which can be replaced by hydrogen by hydrolysis, or an alkali metal derivative thereof, if necessary hydrolysing the product obtained to convert the radical Z1. into hydrogen, optionally converting a product obtained, in which Z is hydrogen, into a product in which Z is a C 1-4 alkyl, C 1-4 hydroxyalkyl or C 3-9 alkanoyloxyalkyl group, or acylating a product in which Z is C 1-4 hydroxyalkyl, into one in which Z is C 3-9 alkanoyloxyalkyl, or hydrolysing a product obtained in which Z is C 3-9 alkanoyloxyalkyl into one in which Z is C 1-4 hydroxyalkyl, and if desired, converting a compound of Formula (I) obtained into an acid addition salt. Starting materials of Formula (II), in which Q is chlorine, are prepared by reacting a compound of Formula (IV) with phosphorus pentachloride. The compound of Formula (II), in which X is hydrogen and Q is ethoxy, is prepared by reacting the corresponding compound, in which Q is chlorine, with ethanol. Thieno - benzothiorepinones of Formula (IV) are prepared by reacting 2-amino-thiophenol or 2-amino-4-chloro-thiophenol with 3-bromothiophene to give a (3-thienylthio)-aniline, reacting this with phosgene to give a (3-thienylthio)-phenyl isocyanate and cyclizing this using aluminium chloride. Pharmaceutical compositions having a central depressant action, for oral, rectal or parenteral administration, comprise a compound of Formula (I), or a pharmaceutically acceptable acid addition salt thereof, together with a carrier.