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Title:
AN AMINO ALCOHOL LIGAND AND ITS USE IN PREPARATION OF CHIRAL PROPARGLIC TERTIARY ALKOHOLS AND TERTIARY AMINES VIA ENANTIOSELECTIVE ADDITON REACTION
Document Type and Number:
WIPO Patent Application WO/2004/087628
Kind Code:
A1
Abstract:
This invention relates to a process of asymmerically alkynating ketones or ketoimines by asymmerical addition of terminal alkynes to trifluoromethyl ketones or trifluoromethyl ketoimines in the presence of copper or zinc salt and a kind of chinal ligand, to form chinal proparglic tertiary alkohols or tertiary amines, which are the key intermediates for preparing new anti-HIV transcriptase inhibitors Efavirenz(DMP 266), DPC 961 and DPC 083. It also relates to a new chinal amino alcohol ligand.

Inventors:
JIANG BIAO (CN)
SI YUGUI (CN)
Application Number:
PCT/CN2003/000462
Publication Date:
October 14, 2004
Filing Date:
June 16, 2003
Export Citation:
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Assignee:
SHANGHAI INST ORGANIC CHEM (CN)
JIANG BIAO (CN)
SI YUGUI (CN)
International Classes:
C07C29/42; C07C213/02; C07C217/48; C07D239/80; C07C215/68; (IPC1-7): C07C33/042; C07C29/42; C07C215/36; C07D239/80
Domestic Patent References:
WO2001070707A22001-09-27
Foreign References:
CN1314333A2001-09-26
CN1185146A1998-06-17
US5202484A1993-04-13
Other References:
See also references of EP 1614672A4
JIANG B. ET AL., CHEM. COMMUN., 2002, pages 1524 - 1525
J. W. CORBETT ET AL., ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1999, pages 2893 - 2897
Attorney, Agent or Firm:
SHANGHAI ZHI XIN PATENT AGENT LTD (446 Zhao Jia Bang Road, Shanghai 1, CN)
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