PROCESS FOR PRODUCING a-FLUORO-ß-AMINO ACIDS

摘要

By reacting a ß-hydroxy-a-amino acid with sulphuryl fluoride (SO2F2) in the presence of an organic base, it is possible to produce an a-fluoro-ß-amino acid represented by formula [2]. [2] By using a C8-12 tertiary amine having two or more alkyl groups of C3 or higher, and especially diisopropylethylamine, as an organic base, by-production of quaternary 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 on an industrial scale.