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Title:
A PROCESS FOR THE PREPARATION OF 2,2-DISUBSTITUTED PYRROLES
Document Type and Number:
WIPO Patent Application WO2005102996
Kind Code:
A3
Abstract:
The present invention relates to the stereoselective preparation of 2,2-disubstituted-4-carbonatepyrroles from readily available chiral starting materials. Such pyrroles are useful as intermediates in the preparation of 2,2,4-trisubstituted 2,5-dihydropyrroles, that are inhibitors of mitotic kinesins and are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The product of the process of the invention may be illustrated by the Formula (I).

Inventors:
JAVADI GARY (US)
KARADY SANDOR (US)
MAEDA KENJI (JP)
MILLER ROSS A (US)
SZUMIGALA RONALD H (US)
Application Number:
PCT/US2005/013630
Publication Date:
January 19, 2006
Filing Date:
April 15, 2005
Export Citation:
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Assignee:
MERCK & CO INC (US)
JAVADI GARY (US)
KARADY SANDOR (US)
MAEDA KENJI (JP)
MILLER ROSS A (US)
SZUMIGALA RONALD H (US)
International Classes:
C07D207/36; (IPC1-7): C07D207/16; C07D211/58; C07D263/04; C07D263/52
Domestic Patent References:
WO2005019206A12005-03-03
WO2004037171A22004-05-06
Foreign References:
US20050038074A12005-02-17
Other References:
WIPF P. AND STEPHENSON C. ET AL: "Dimethylzinc-Mediated Addition of Alkenylzirconocenes to Alpha-Keto and Alpha-Imino Esters.", ORG LETT., vol. 5, no. 14, 2003, pages 2449 - 2452, XP002990772
MA D. ET AL: "Asymetric synthesis of (s)-1 aminoindian-1,5-dicarboxylic acid and related analogues via intramolecular acylation of enantiopure alpha-alpha-disubstituted amino acids.", TETRAHEDRON: ASYMMETRY., vol. 13, June 2002 (2002-06-01), pages 961 - 969, XP004365920
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