Patent ID: 7790927

Claim:
A process for the production of an optically active 2-aryl cyclopropylamine compound represented by general formula (9), or a salt thereof, wherein * denotes an asymmetric carbon centre, and wherein an optically active 2-aryl cyclopropanecarboxylic acid compound represented by general formula (7), wherein * denotes an asymmetric carbon centre, is obtained, by de-esterifying an optically active 2-arylcyclopropane carboxylate ester compound represented by general formula (6) wherein R 5 is an optionally substituted C 1-10 cyclic or acyclic alkyl group, optionally substituted C 6-10 aryl group, or optionally substituted C 7-10 aralkyl group, and * denotes an asymmetric carbon centre, and wherein the compound of formula (6) is obtained by reacting an optically active styrene oxide compound represented by general formula (3) wherein * denotes an asymmetric carbon centre, or optically active halohydrin compound represented by general formula (4) wherein X denotes a halogen atom, and * denotes an asymmetric carbon centre, with a phosphonoacetic acid ester compound represented by general formula (5) wherein each R 5 and R 6 is, independently, a substituted C 1-10 cyclic or acyclic alkyl group, optionally substituted C 6-10 aryl group, or optionally substituted C 7-10 aralkyl group, in the presence of base; and thereafter, the 2-aryl cyclopropanecarboxylic acid compound of formula (7) obtained is activated by reaction with a carboxylic acid activator and thereafter reacting with ammonia to give the optically active 2-aryl cyclopropane carboxamide compound represented by obtained general formula (8) wherein * denotes an asymmetric carbon centre, which is reacted with an oxidant to give the compound of formula (9).