| 摘要 |
<p>1,269,404. 1-Substituted-2,5-diphenylpyrroles. A. H. ROBINS CO. Inc. 19 June, 1969 [21 June, 1968], No. 31037/69. Heading C2C. Novel 1 - substituted - 2,5 - diphenyl-pyrroles of the general formula wherein R is an amino, hydroxy, 1,2-dihydroxyethyl, 1,3-dioxolan-2-on-4-yl, aryloxy, optionally N-substituted carbamoyloxy, morpholinyl, N - acylpiperidinyl - 4 - carbonyloxy, 1 - acylpiperazinyl - 4 - carbonyloxy, pyrrolidinyl or piperidinyl group, R<SP>1</SP> is a hydrogen, fluorine, chlorine or bromine atom or a C 1-8 alkyl, C 1-8 alkoxy or trifluoromethyl group, and n is an integer from 1 to 5 inclusive, and acid addition salts thereof are prepared (a) by reaction of a 2,5-diphenyl-pyrrole of the general formula with a compound of the general formula X(CH 2 ) n R, wherein X is a halogen atom; (b) by reaction of a 1,2-dibenzoylethane of the general formula with an amine of the general formula NH 2 (CH 2 ) n R; (c) when R is a 1,3-dioxolan-2- on-4-yl group, by reaction of the corresponding compound wherein R is a 1,2-dihydroxyethyl group with phosgene; (d) when R is an N-alkylcarbamoyloxy group, by reaction of the corresponding compound wherein R is a hydroxy group with an alkyl isocyanate; (e) when R is a 1-acyl-4-piperidinylcarbonyloxy group, by reaction of the corresponding compound, wherein R is a hydroxy group with 1-acyl-isonipecotic acid halide; and (f) when R is a 1-acyl-4- piperazinylcarbonyloxy group, by reaction of the corresponding compound wherein R is a hydroxy group with 4-halocarbonyl-1-acylpiperazine; followed optionally by salification of the product. Pharmaceutical compositions having analgesic activity comprise, as active ingredient, a 1- substituted-2,5-diphenyl-pyrrole of the first general formula above or a non-toxic acid addition salt thereof, together with a pharmaceutically acceptable carrier, and may be administered orally or parenterally.</p> |
