Hydrochloric Acid → HCID 66954873, compound

Participants

Reaction Steps

A preferred aspect of the invention is a process for the preparation of (S)-methyl 2-amino-5-cyclopropyl-4,4-difluoropentanoate hydrochloride, which process comprises: (a) reacting (R,S)-ethyl 2-(tert-butoxycarbonylamino)-5-cyclopropyl-4,4-difluoropentanoate with Alcalase to give a mixture of (R)-ethyl 2-(tert-butoxycarbonylamino)-5-cyclopropyl-4,4-difluoropentanoate and (S)-2-(tert-butoxycarbonylamino)-5-cyclopropyl-4,4-difluoropentanoic acid; (b) isolating the (S)-2-(tert-butoxycarbonylamino)-5-cyclopropyl-4,4-difluoropentanoic acid; (c) deprotecting the (S)-2-(tert-butoxycarbonylamino)-5-cyclopropyl-4,4-difluoropentanoic acid with hydrochloric acid to give (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid hydrochloride; and (d) treating the (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid hydrochloride with methanol.

Provenance & Evidence