Novel process for...

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C - Chemistry, Metallurgy

07

D

C07D 405/06 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61K 31/535 (2006.01) C07B 41/00 (2006.01) C07B 43/00 (2006.01) C07C 255/29 (2006.01) C07D 207/327 (2006.01) C07D 207/34 (2006.01) C07D 295/185 (2006.01) C07D 319/06 (2006.01) C07D 401/06 (2006.01) C07D 403/06 (2006.01) C07D 405/14 (2006.01) C07D 413/00 (2006.01)

Patent

CA 2155952

An improved process for the preparation of trans- 6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones having the following general structural formula I (see formula I) 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-methyl-fc ethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H- pyran-2-yl)ethyl]-1H-pyrrol-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.

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