| 摘要 |
<p>[PROBLEMS] To provide an industrially advantageous process for production of (3R,4S)-3-cyclopropylaminomethyl-4- fluoropyridine or an enantiomer thereof, which is a useful intermediate for the production of a 10-(3-cyclopropylaminomethyl-4-fluoropyrrolidinyl)- pyridobenzoxazinecarboxylic acid derivative which is a novel antibacterial agent. [MEANS FOR SOLVING PROBLEMS] A novel substance (3R,4S)-1-protected-3-cyclopropylcarbamoyl-4-hydroxy- pyrrolidine or an enantiomer thereof having a high optical purity can be produced by performing the highly stereoselective asymmetric hydrogenation of a 1-protected-4-alkoxycarbonyl-3-oxopyrrolidine, performing the ester hydrolysis, and then performing the amidation with cyclopropylamine to produce a crude crystal, and recrystallizing the crude crystal. By using this compound as an intermediate, it becomes possible to establish an industrial production process for producing (3R,4S)-3-cyclopropylaminomethyl-4- fluoropyrrolidine having a high quality or an enantiomer thereof by means of simple procedures at a high purity and in a steady yield.</p> |
