GB1332737A - Process for producing butyrophenone derivatives - Google Patents

Abstract

1332737 Piperazino-butyrophenone derivatives SUMITOMO CHEMICAL CO Ltd 19 April 1971 [6 March 1970 14 May 1970] 23304/71 Heading C2C Compounds I in which R<SP>1</SP> is H, halo, NH 2 , 1-4 C alkylamino, acylamino or N-(1-4 C alkyl)-amino; R<SP>2</SP> is H or halo; R<SP>3</SP> is H, halo, 1-4 C alkyl, 1-4 C alkoxy or CF 3 and n is 0, 1 or 2 and acid addition salts thereof are prepared by oxidation of compounds V to give compounds II and optional hydrolysis of compounds II to give compounds III and, if R<SP>5</SP> is H, optional diazotization of compounds III followed by decomposition of the diazonium compound to give compounds IV in which X is H or halo. Compounds I in which R<SP>1</SP> is other than H and compounds I in which R<SP>1</SP> is H and R<SP>2</SP> is halo in the meta position are claimed per se. Compounds V may be prepared by reaction of compounds VII with R<SP>6</SP>MgHal (R<SP>6</SP> is 1-5 C alkyl) followed by reaction of the Grignard reagents with compounds X or by reduction of compounds VI Compounds VI may be prepared by reaction of compounds VIII or their functional derivatives with compounds XII by oyclization of compounds IX or by reaction of the Grignard reagents prepared from compounds VII with compounds XI Pharmaceutical compositions comprise one of the above-mentioned novel compounds and a suitable carrier and have central nervous system activity. Reference has been directed by the Comptroller to Specification 1,180,864.