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Title:
METHODS FOR THE SYNTHESIS OF MILNACIPRAN AND CONGENERS THEREOF
Document Type and Number:
WIPO Patent Application WO2005118564
Kind Code:
A3
Abstract:
One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

Inventors:
BUCHWALD STEPHEN L (US)
SWAGER TIMOTHY M (US)
RARIY ROMAN V (US)
Application Number:
US2005011365W
Publication Date:
April 27, 2006
Filing Date:
April 01, 2005
Export Citation:
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Assignee:
COLLEGIUM PHARMACEUTICAL, INC.
BUCHWALD, STEPHEN, L.
SWAGER, TIMOTHY, M.
RARIY, ROMAN, V.
International Classes:
A61K31/195; C07C61/16; C07D209/48; C07D307/00; (IPC1-7): C07D307/00
Other References:
GIUSSEPPE RONNISVALLE ET AL.: "Substituted 1-Phenyl-2-cyclopropylmethylamines with High Affinity and Selectivity for Sigma Sites" BIOORGANIC & MEDICINAL CHEMISTRY, vol. 8, 2000, pages 1503-1513, XP002348657
BERNARD BONNAUD ET AL.: "Synthesis of Novel Indolizine Derivatives" J. HETEROCYCLIC CHEM., vol. 28, 1991, pages 1927-1932, XP002348658
BERNARD BONNAUD ET AL.: "1-Aryl-2-(aminomethyl)cyclopropanecarboxy lic Acid Derivatives. A New series of antidepressants" J. MED. CHEM., vol. 30, 1987, pages 318-325, XP002348659
SHUTO S ET AL: "Synthesis of (+)- and (-)-milnaciprans and their conformationally restricted analogs" 29 January 1996 (1996-01-29), TETRAHEDRON LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, PAGE(S) 641-644 , XP004030321 ISSN: 0040-4039 Scheme 2, step g the whole document
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