| 摘要 |
<p>1,212,149. Heterocyclic derivatives of 2-(paminoaryl) ethanol. E. MERCK A.G. 26 June, 1969 [1 Aug., 1968], No. 32342/69. Heading C2C. The invention comprises compounds of formula wherein R<SP>1</SP> is OH (which may be esterified or etherified), R<SP>2</SP> is H, Me or Et, R<SP>3</SP> is F, Cl, Br, I, NO 2 , NH 2 , Me, Et, MeS when R<SP>4</SP> and R<SP>5</SP> are H, or R<SP>3</SP> is H when R<SP>4</SP>, R<SP>5</SP> together form -CH=CH-CH=CH-, and Q is pyrrolidino, piperidino or homopiperidino; and their acid addition and quaternary ammonium salts. Standard preparative methods are used. Specified intermediates corresponding with the above formula are prepared, which may have (a) instead of the -CHR<SP>2</SP>CH<SP>2</SP>R<SP>1</SP> group: CHMeCOCl, C(: CH 2 )COCl, CHMeCHO, CHR<SP>2</SP>CO 2 R<SP>2</SP>, CMe: CHOMe, CHClCH 2 OMe, CMe 2 OH, COCH 2 Br, CHMeCO 2 CO 2 Et, CHR<SP>2</SP>CH 2 Br, CMe: CH 2 , COCH 2 OMe, CHOHCH 2 OH, CHMeOH, C(: CH 2 )CH 2 OMe, C(OH)MeCH 2 OMe, Ac, CMeCH 2 O, CHMeCON 3 , CHMeCONHNH 2 , CHMeCH 2 NH 2 ; and/or (b) instead of R<SP>3</SP>: CN, Ac or SH, or instead of R<SP>4</SP>R<SP>5</SP>: -(CH 2 ) 4 - or H for R<SP>3</SP>, R<SP>4</SP>, R<SP>5</SP>; and/or (c) instead of Q: Br, NH 2 , MeCONH, Br(CH 2 ) 4 CONH or 2-(hydroxy, methoxy or oxo) piperidino. Also prepared is 2-(3-chloro-4- piperidinophenyl) propyl carbonate. Therapeutic compositions for parenteral, enteral or topical application comprise compounds of the above formula, which have antiphlogistic, analgesic, antipyretic, bacteriostatic, bactericidal, antiprotozoal, diuretic, hypoglycaemic, choleretic, hypocholesterolaemic and antiradiation activity.</p> |
