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

Details Process for trans-6-[2-(substituted-pyrrol-1-yl) alkyl]... Process for trans-6-[2-(substituted-pyrrol-1-yl) alkyl]...

C - Chemistry, Metallurgy

07

D

260/326, 260/351

C07D 319/06 (2006.01) C07C 235/80 (2006.01) C07D 207/34 (2006.01) C07D 319/08 (2006.01) C07D 405/06 (2006.01) C07D 405/14 (2006.01)

Patent

CA 1330441

ABSTRACT An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien- 4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(?)-5-(4-fluoro- phenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro- 4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3- carboxamide by a novel synthesis where 4-methyl-3-oxo- N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-.alpha.-[2- methyl-1-oxopropyl]-?-oxo-N,.beta.-diphenylbenzenebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5- (4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2- (tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H- pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1- dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.

590367

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