PROCESS FOR PREPARING ENANTIOMERICALLY ENRICHED 3-HYDROXYMETHYLPIPERIDINE

摘要

The present invention relates to a process for preparing enantiomerically enriched 3-hydroxymethylpiperidine and in particular of the S-enantiomer of (S)-3-hydroxymethyl-piperidine in high chemical and optical purity. The invention also relates to extremely pure (S)-3-hydroxymethylpiperidine and (R)-3-hydroxymethylpiperidine.

主权项

1. A process for preparing enantiomerically enriched 3-hydroxymethylpiperidine, which comprises the following steps:
a) providing enantiomerically enriched piperidine-3-carboxylic acid or an enantiomerically enriched ester of piperidine-3-carboxylic acid, b) reduction of the enantiomerically enriched piperidine-3-carboxylic acid or its ester with a boron containing reducing agent to yield a reaction mixture containing enantiomerically enriched 3-hydroxymethylpiperidine; and c) aqueous work-up of the reaction mixture; where the boron containing reducing agent is selected from the group consisting of BH3, complexes of BH3, mixtures of a tetrahydroborate salt with a metal salt of group 2, 4 or 12 metals and tetrahydroborates of group 2, 4 or 12 metals, and mixtures thereof.