Efficient stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines and intermediates thereto

摘要

Stereoconservative method for preparation of an (R)- or (S)-isomer of the compound of the formula I with at least 95% optical purity (* CHEMICAL STRUCTURE *) (I) wherein R1 is a hydrogen atom, a saturated or unsaturated lower alkyl group, a cycloalkyl group, or a group (CH2)m Ph wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group including 1) O,N-dialkylation, directly or stepwise of (R)- or (S)-proline 2) aminolysis 3) reduction to formation of the (R)- or (S)-isomer of the compound of the formula I, and new intermediates II and III in optical active form obtained by the reaction steps above and wherein R2 is defined as R1 above. (* CHEMICAL STRUCTURE *) (II) (* CHEMICAL STRUCTURE *) (III)