申请人:Ishii Akihiro
公开号:US20110015428A1
公开(公告)日:2011-01-20
By reacting a β-hydroxy-α-amino acid with sulfuryl fluoride (SO
2
F
2
) 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.