METHOD FOR PRODUCING (2S, 4S)-1-HYDROXYACETYL-2-AMINOCARBONYL-4-FLUOROPYRROLIDINE

摘要

According to the invention, (2S, 4R)-2-alkoxycarbonyl-4-hydroxypyrrolidine or an acid salt thereof is reacted with an alkylcarbonyloxyacetyl halide in the presence of a base and thereby converted to (2S, 4R)-1-alkylcarbonyloxyacetyl-2-alkoxycarbonyl-4-hydroxypyrrolidine, the product is then reacted with a dehydroxyfluorination agent and thereby converted to (2S, 4S)-1-alkylcarbonyloxyacetyl-2-alkoxycarbonyl-4-fluoropyrrolidine, and the product is reacted with ammonia to eventually obtain (2S, 4S)-1-hydroxyacetyl-2-aminocarbonyl-4-fluoropyrrolidine. The invention is useful as an industrial production method with which the number of reaction steps of the conventional production method can be particularly reduced and the title compound can be supplied with high productivity and inexpensively.