Warner-lambert Company

Tung V Le

Donald E Butler

Thomas N Nanninga

David Juergen Wustrow

Alan Millar

Jodette Gailey

William John Smith, Iii

An improved process for the preparation of R(+)1,2,3,6-tetrahydro-4-phenyl-1-�(3-phenyl-3-cyclohexen-1-yl)methyl!pyri dine by a novel synthesis is described where 5-oxo-3-phenyl-3-cyclohexene-carboxylic acid is converted in five operations to the desired product, as well as processes for the resolution of 5-oxo-3-phenyl-3-cyclohexenecarboxylic acid using cinchonidine to afford (S)5-oxo-3-phenyl-3-cyclohexenecarboylic acid or .alpha.-chymotrypsin to selectively hydrolyze n-butyl 5-oxo-3-phenyl-3-cycohexenecarboxylate to afford (S)5-oxo-3-phenyl-3-cyclohexenecarboxylic acid as well as other valuable intermediates used in the processes.

Process for R (+)

An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pyran-2-one

Process for trans-6[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one

An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one

An improved process for the preparation of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate is described where a halo hydroxyester or other activated dihydroxyester is converted in two steps to the desired product.

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Jenison, MI, United States of America

Tung V Le