Invention Grant
US5124482A Process for trans-6-(2-substituted-pyrrol-1-yl)alkyl)pyran-2-one
inhibitors of cholesterol synthesis
失效
反式-6-(2-取代 - 吡咯-1-基)烷基)吡喃-2-酮胆固醇合成抑制剂的方法
- Patent Title: Process for trans-6-(2-substituted-pyrrol-1-yl)alkyl)pyran-2-one inhibitors of cholesterol synthesis
- Patent Title (中): 反式-6-(2-取代 - 吡咯-1-基)烷基)吡喃-2-酮胆固醇合成抑制剂的方法
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Application No.: US792311Application Date: 1991-11-14
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Publication No.: US5124482APublication Date: 1992-06-23
- Inventor: Donald E. Butler , Carl F. Deering , Alan Millar , Thomas N. Nanninga , Bruce D. Roth
- Applicant: Donald E. Butler , Carl F. Deering , Alan Millar , Thomas N. Nanninga , Bruce D. Roth
- Applicant Address: NJ Morris Plains
- Assignee: Warner-Lambert Company
- Current Assignee: Warner-Lambert Company
- Current Assignee Address: NJ Morris Plains
- Main IPC: C07C235/80
- IPC: C07C235/80 ; C07D207/34 ; C07D319/06 ; C07D319/08 ; C07D405/06
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-fluorophenyl)-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]-.gamma.-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.
Public/Granted literature
- US5698736A High temperature, catalytic Friedel-Crafts synthesis of benzene phosphorus dichloride Public/Granted day:1997-12-16
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