Solvent and in situ catalyst preparation impacts upon Noyori reductions of aryl-chloromethyl ketones: application to syntheses of chiral 2-amino-1-aryl-ethanols
摘要:
As part of medicinal chemistry efforts we found it necessary to develop general syntheses of highly enantiomerically enriched 1-aryl-2-chloroethanols and 1-aryl-2-methylaminoethanols. A survey of literature methods suggested that a truly general approach had not yet been reported, encouraging us to undertake the development of such a methodology. This study describes the design, development, and reduction to practice of a general synthesis of chiral 1-aryl-2-chloroethanols and the transformation of these entities to highly enantiomerically enriched 1-aryl-2-methylaminoethanols. Of particular importance were observations of the impact of solvent and the method of catalyst preparation on the yield and enantiomerical excess of chlorohydrins prepared via Noyori transfer hydrogenations of aryl-chloromethyl ketones. (c) 2006 Elsevier Ltd. All rights reserved.
OXOTHIENO[3,2-B]PYRIDINECARBOXAMIDES AS ANTIVIRAL AGENTS
申请人:PHARMACIA & UPJOHN COMPANY
公开号:EP1467999A1
公开(公告)日:2004-10-20
THIENO(3,2-B)PYRIDONES AS ANTIVIRAL COMPOUNDS
申请人:PHARMACIA & UPJOHN COMPANY
公开号:EP1472260A2
公开(公告)日:2004-11-03
[EN] PYRIDOQUINOXALINE ANTIVIRALS<br/>[FR] ANTIVIRAUX A BASE DE PYRIDOQUINOXALINE
申请人:UPJOHN CO
公开号:WO2003053971A1
公开(公告)日:2003-07-03
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein R?1, R2 and R3¿ are as defined in the specification. The compounds are useful for the treatment of viral infections.