The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jul. 10, 2012

Filed:

Apr. 21, 2009
Applicants:

Akihiro Ishii, Kawagoe, JP;

Takako Yamazaki, Kawagoe, JP;

Manabu Yasumoto, Kawagoe, JP;

Takashi Masuda, Kawagoe, JP;

Hideyuki Tsuruta, Fujimino, JP;

Inventors:

Akihiro Ishii, Kawagoe, JP;

Takako Yamazaki, Kawagoe, JP;

Manabu Yasumoto, Kawagoe, JP;

Takashi Masuda, Kawagoe, JP;

Hideyuki Tsuruta, Fujimino, JP;

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07C 227/16 (2006.01);
U.S. Cl.
CPC ...
Abstract

By reacting a β-hydroxy-α-amino acid with sulfuryl fluoride (SOF) in the presence of an organic base, it is possible to produce an α-fluoro-β-amino acid of the formula [2]. By using a C8-12 tertiary amine having two or more alkyl groups of C3 or higher, and especially diisopropylethylamine, as the organic base, by-production of quantery ammonium salts is effectively suppressed. By applying the production process of the present invention, it is possible to very easily produce (2R)-3-(dibenzylamino)-2-fluoropropionic acid methyl ester, which is extremely important as a pharmaceutical intermediate, with high positional selectivity even on an industrial scale.


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