PHENOXY SUBSTITUTED PHENYLACETIC ACIDS

专利名称：PHENOXY SUBSTITUTED PHENYLACETIC

ACIDS

发明人：WILLIAM A. BOLHOFER申请号：US58394066申请日：19661003公开号：US3517051A公开日：19700623

摘要：New compounds of the general formula wherein either (1) A is oxygen, Y isphenyl, unsubstituted or with one or two similar or dissimilar substituents from amonghalogen, C1- 5 alkyl, haloalkyl (inc. CF3), C1- 5 alkoxy, C1- 6 alkanoyl, aryl, aralkyl, aryloxy,aralkoxy, cyano, carboxy and C1- 5 alkylsulfonyl, m is 1, 2 or 3, and R1 is similar is C2- 5alkenyl, haloalkyl, C1- 6 alkanoyl, aryl, aralkyl, aralkenyl, aryloxy, aralkoxy, arylthio,arylamino, carboxy, C1- 5 alkylthio, C1- 5 alkylsulfonyl, cyano, nitroso, amino,

monoalkylamino or dialkylamino; or (2) A is oxygen or sulphur, Y is benzyl or phenethyl,unsubstituted or with one or two similar or dissimilar substituents from among halogen,C1- 5 alkyl and C1- 5 alkoxy, m is 1, and R1 is halogen or as above) are prepared byreaction of compounds (R1)mPh-AM (where M is alkali metal) with compounds X-CHY-COOR12 where X is halogen and R12 is hydrocarbyl, followed by hydrolysis of thehydrocarbyl esters (carboxy groups R1 may be simultaneously formed by hydrolysis ofalkoxy-carbonyl-substituted precursors). The acids may be converted to salts withinorganic and organic bases; the invention also includes alkyl esters of the acids.

Haloesters X-CHY-COOR12 are formed from compounds YCH2-COOH by forming YCH2-COCl, halogenating to X-CHY-COCl and then reacting with R12OH. Pharmaceutical

compositions comprise the new compounds with carriers, oral and parenteralcompositions of these hypocholesteremic agents being described.

申请人：MERCK & CO. INC.

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