GB1069731A - Phenthiazine derivatives and pharmaceutical compositions containing same - Google Patents

Abstract

The invention comprises compounds of the general Formula (I) <FORM:1069731/C2/1> wherein R1 represents a C2 to C6 alkyl radical or an aryl or aralkyl radical and R2 represents a hydrogen atom or a C1 to C4 alkyl radical, and their acid addition salts. Said compounds may be prepared by reacting a compound of the Formula (II) <FORM:1069731/C2/2> wherein Hal represents a chlorine or bromine atom, with 4-hydroxy-piperidine at an elevated temperature in an organic solvent therefor and in the presence of an acid-binding agent and, when an acid-addition salt is desired, salification is effected with an organic or inorganic acid. An excess of the 4-hydroxy-piperidine may provide the acid-binding agent. Compounds of Formula (II) wherein Hal is chlorine may be prepared by refluxing a compound of Formula (III) <FORM:1069731/C2/3> at 180 DEG C. with sodium amide in xylene and adding 1-bromo-3-chloropropane to the reaction mixture at 40 DEG C. prior to further heating at 180 DEG C. The compounds of Formula (I) and their physiologically acceptable acid addition salts are pharmaceutically active having sedative/neuroleptic properties, cataleptic activity, adrenolytic action and hypotensive action and may be employed, together with physiologically acceptable carriers, in oral or parential preparations.