PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY ENRICHED 3-AMINOPIPERIDINE

摘要

The present invention relates to a process for the preparation of enantiomerically enriched 3-aminopiperidine, and in particular of its R-enantiomer (R)-3-aminopiperidine. The invention also relates to an enantiomerically enriched intermediate of said process and to specific acid-addition salts of 3-aminopiperidine (hereinafter also APIP) that are useful for obtaining a single enantiomer of APIP, and to crystalline (R)-3-aminopiperidine-dihydrochloride-monohydrate and crystalline (S)-3-aminopiperidine-di-hydrochloride-monohydrate.

主权项

1. A process for preparing 3-aminopiperidine, which process comprises the following steps:
a) providing piperidine-3-carboxylic acid hydrazide, and b) transforming piperidine-3-carboxylic acid hydrazide into the piperidine-3-carbonyl azide and c) reacting piperidine-3-carbonyl azide in the presence of water and an acid.