GB988008A - - Google Patents

Abstract

988,008. Dibenzothiazepine derivatives. RHONE-POULENC S.A. May 15, 1962 [May 15, 1961; March 20, 1962], No. 18719/62. Heading C2C. The invention comprises bases of the general formula (wherein A represents a straight or branched chain C 2-6 alkylene group with at least 2 carbon atoms between the nucleus and the group Z, and Z represents an amino or mono- or di-alkylamino group or a 4-, 5- or 6-membered nitrogencontaining heterocyclic group attached to A by a nitrogen atom) and their non-toxic acid addition and quaternary ammonium salts, and pharmaceutical compositions containing these compounds in association with a pharmaceutical carrier or coating, and the preparation of the bases by reacting 6,11-dihydro-dibenzo- [b,e][l,4]-thiazepine (II) with a reactive ester of an alcohol Z-A-OH, or by decarboxylating an ester of the general formula by heating above 100‹ C. until evolution of carbon dioxide ceases. The bases can also be prepared by reacting a compound of formula (I), wherein Z represents the acid residue of a reactive ester, with a compound H-Z. Esters (III) are prepared by reacting (II) with phosgene and reacting the resulting carboxylic chloride (or other halide or a corresponding carboxylic ester) with an alcohol Z-A-OH. 6,11 - Dihydrodibenzo - [b,e][1,4] - thiazepine (II) is prepared by cyclizing 2-aminophenyl 2<SP>1</SP>- bromobenzyl sulphide by heating it in the presence of anhydrous potassium carbonate and copper powder. The pharmaceutical compositions, which have antidepressant and, in some cases, spasmolytic activity, may be in forms suitable for oral or parenteral administration, e.g. tablets, pills, dispersible powders, granules, emulsions, solutions, suspensions, syrups or elixirs. Acid addition salts specified include theophyllinates, theophyllinacetates, salicylates, phenolphthalinates and methylene -bis-(p-hydroxynaphthoates).