PRODUCTION OF 3-AMINO-4-METHYLENE PYRROLIDINE DERIVATIVE

摘要

PURPOSE:To industrially and advantageously produce the title compound by using an 3-amino-4-oxopyrrolidine derivative as a starting raw material and subjecting the above-mentioned derivative to methylene formation without using harmful and specific reagent and simply and safely introducing a methylene side chain at the 4-position thereof. CONSTITUTION:An 3-amino-4-oxopyrrolidine derivative [e.g. 1-tert. butoxycarbonyl-N-methyl) amino-4-oxopyrrolidine] expressed by formula I (R<1> and R<3> are amino-protecting groups; R<2> is H or lower alkyl) is subjected to methylene formation to provide 3-amino-4-methylenepyrrolidine derivative [1-tert. butoxycarbonyl-3-(N-methoxycarbonyl-N-methyl) amino-4-methylenepyrrolidine]. A compound expressed by the formula (C6H5)P=CH2 is used as an exomethylene-forming reagent of the ketone body expressed by formula I. The compound expressed by formula I is useful as a pyrrolidine derivative capable of forming 7 position of pyridonecarboxylic acid which is an antimicrobial agent.