| 摘要 |
<p>Provided is a process for preparing, with industrial advantages and at a low cost, optically active syn-3-(N-substituted -aminomethyl)-4-fluoropyrrolidines which can serve as intermediates in the preparation of drugs. More specifically disclosed is a process for the preparation of syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivatives, enantiomers thereof, or salts of the same, which includes a step of fluorinating a compound represented by general formula (6) or an enantiomer thereof with both a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure. In general formula (6), PG1 is an amino-protecting group; R1 is optionally substituted C1-6 alkyl or optionally substituted C3-8 cycloalkyl; and Ns is a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group.</p> |
