| 摘要 |
1288670 2 - (4 - Halophenoxy) - alkanoic acid esters MERCK & CO Inc 4 Aug 1970 37621/70 Heading C2C Novel 2 - (4 - halophenoxy) - alkanoic acid esters of the general formula wherein R is a (C 1-6 alkanoylamino)alkyl, benzamidoalkyl, ureidoalkyl, N<SP>1</SP> - alkylureidoalkyl or N<SP>1</SP>,N<SP>1</SP> - dialkylureidoalkyl group or a phenacyl group optionally substituted by a single halogen atom or alkyl or alkoxy group in the benzene ring, R<SP>1</SP> and R<SP>2</SP> are each an alkyl group or R<SP>1</SP> and R<SP>2</SP>, together with the carbon atom to which they are attached, form a cylcohexane ring, X is a halogen atom and all the alkyl and alkoxy groups mentioned contain 1-5 carbon atoms, are prepared (a) by reaction of a 2-(4-halophenoxy)-alkanoic acid halide of the general formula wherein X<SP>1</SP> is a halogen atom, with an alkanol of the general formula ROH; or (b) when R is an optionally substituted phenacyl group, by reaction of a 2-(4-halophenoxy)-alkanoic acid of the general formula with a phenacyl halide of the general formula R<SP>5</SP>X<SP>1</SP>, wherein R<SP>5</SP> is a phenacyl group optionally substituted by a single halogen atom or C 1-5 alkyl or C 1-5 alkoxy group in the benzene ring, in the presence of a base. Pharmaceutical compositions having hypocholesterolemic and hypolipemic activity comprise, as active ingredient, a 2-(4-halophenoxy)- alkanoic acid ester of the first general formula above, together with a pharmaceutical vehicle, and may be administered orally or intravenously. |
