1,4-SUBSTITUTED PHENYL PIPERAZINE

摘要

1,266,780. 2-Phenylpiperazine and 2-phenyl- 3-piperazinone derivatives. DONAU-PHARMAZIE G.m.b.H. 24 July, 1969 [26 July, 1968], No. 37313/69. Heading C2C. The invention comprises compounds of formula wherein X, Y and Z are each H, halogen, OH or C 1-5 alkoxy (possibly Ph-substituted), n is 1-3, R is di-(C 1-5 alkyl)-amino-C 1-5 alkyl, or is C 1-5 alkyl substituted by piperidino, pyrrolidino, piperazino, 4-C 1-5 -alkylpiperazino, 3-ketopiperazino or morpholino, and A-B is -PhCH-CO-, -PhCH-CH 2 -, -CO-CHPh- or -CH 2 -CHPh-, and their pharmaceutically acceptable acid addition salts. These compounds are prepared by (a) reducing the 1,4-disubstituted phenylpiperazinones to the phenylpiperazines, or (b) reacting together the appropriate (i) aralkyl halide and 1-R-phenylpiperazinone or 1-R- phenylpiperazine, (ii) R-halide and 1-aralkylphenylpiperazinone or 1-aralkylphenylpiperazine, (iii) R1H and 1-aralkyl-4-haloalkylpiperazinone or 1-aralkyl-4-haloalkylpiperazine. Starting materials otherwise prepared are 1-pchlorobenzyl - 2 - phenyl - 4 - acetoxyacetyl (and 21-hydroxyethyl)piperazine. Therapeutic compositions for oral, parenteral or rectal administration comprise a pharmaceutical carrier and a compound of the above formula, which is an anticoagulant.