Patent ID: 6153414
Filing Date: 2000-11-28
Classification: C07D,C12P

Abstract:
Method for the racemate resolution of cis- and trans-pyrrolopiperidine, characterized in that a mixture, which comprises (R,R)- and (S,S)-pyrrolopiperidine or (S,R)- and (R,S)-pyrrolopiperidine, is enzymatically monoacylated to give a mixture (I) which comprises (R,R)- and (S,S)-6-acyl-pyrrolopiperidine or (S,R)- and (R,S)-6-acyl-pyrrolopiperidine, this mixture (I) is enzymatically further acylated to give a mixture (II) which comprises (S,S)-1,6-diacyl- and (R,R)-6-acyl-pyrrolipiperidine or (S,R)-1,6-diacyl- and (R,S)-6-acyl-pyrrolopiperidine, the enzyme and optionally solvent and excess acylating agent are separated off from the mixture (II), and the remainder is treated with aqueous acid, and (S,S)-1,6-diacyl-pyrrolopiperidine or (S,R)-1,6-diacyl-pyrrolopiperidine is separated off by extraction, and the extraction residue is rendered alkaline, and (R,R)-6-acyl-pyrrolopiperidine or (R,S)-6-acyl-pyrrolopiperidine is separated off by extraction.