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Title:
METHOD FOR CRYSTALLIZING REVERSE TRANSCRIPTASE INHIBITOR USING ANTI-SOLVENT
Document Type and Number:
Japanese Patent JP2011006472
Kind Code:
A
Abstract:

To provide a Form I crystalline product of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one and a process for producing the crystalline product.

The desired final crystal form, Form I, can be produced from a solvent and anti-solvent system when using methanol or ethanol. Form II is isolated from 2-propanol and can be converted to the desired crystal form at low drying temperatures, such as between about a temperature of 40°C and 50°C.


Inventors:
CLARKE WILLIAM
CROCKER LOUIS S
KUKURA JOSEPH L II
Application Number:
JP2010202879A
Publication Date:
January 13, 2011
Filing Date:
September 10, 2010
Export Citation:
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Assignee:
MERCK SHARP & DOHME
International Classes:
C07D265/18; A61K9/14; C12N9/99; A61K31/536; A61P43/00; B01D9/00; C12N9/00; C07D
Domestic Patent References:
JPH06184124A1994-07-05
Foreign References:
WO1996037457A11996-11-28
WO1996022955A11996-08-01
WO1996037457A11996-11-28
Other References:
JPN6008056725; THOMPSON, A. S., et al.: 'Use of an Ephedrine Alkoxide to Mediate Enantioselective Addition of an Acetylide to a Prochiral Ket' Tetrahedron Lett. 36(49), 1995, pp.8937-8940
Attorney, Agent or Firm:
Yoshio Kawaguchi
Katsuma Osaki



 
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