IP Library Granted Patent US 8,884,019
Granted Patent B2
US 8,884,019 · App. 14/020,286 · Granted Nov 11, 2014

Benzimidazole compound crystal

Inventors: Akira Fujishima (Hyogo, JP); Isao Aoki (Hyogo, JP)
Assignee: Takeda Pharmaceutical Company Limited
C07D401/12A61K31/4439
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Quick Facts
Patent No.
US 8,884,019
App. No.
14/020,286
Granted
Nov 11, 2014
Kind
B2
Abstract

A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.

Claims (7)

1. A method for producing an amorphous of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole or salt thereof, which comprises:

subjecting a racemate of a compound of 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole to an optical resolution so that an R-enantiomer of the compound is obtained;

adding a solvent comprising ethanol to the obtained R-enantiomer of the compound so that the R-enantiomer of the compound dissolves in the solvent and an R-enantiomer solution is formed;

optionally concentrating the R-enantiomer solution so as to form a concentrate;

further adding hexane to the R-enantiomer solution or the concentrate; and

evaporating the resulting solution to dryness.

2. A method according to claim 1 , wherein the optical resolution is carried out by using a chiral column.

Priority Claims (1)
JP 11-171509 · Jun 17, 1999 · national
Continuity (10)
Continuation 13591992 · Aug 22, 2012
Division 13223988 · Sep 1, 2011
Continuation 12771486 · Apr 30, 2010
Continuation 12393409 · Feb 26, 2009
Continuation 12006845 · Jan 7, 2008
Continuation 11149903 · Jun 10, 2005
Continuation 10655114 · Sep 4, 2003
Continuation 10243329 · Sep 13, 2002
Continuation 09674624
Related Publication 20140012006A1 · Jan 9, 2014