METHOD FOR PRODUCING AN OPTICALLY ACTIVE TETRAHYDROQUINOLINE

摘要

The present invention provides an industrially advantageous production method of optically active tetrahydroquinolines of formula (1), which comprises: 1) a step of reacting a beta-ketoester of formula (2) with an amine of formula (3) to produce an enaminoester of formula (4); 2) a step of subjecting the enaminoester of formula (4) above obtained in 1) to asymmetric hydrogenation to produce an optically active beta-amino acid derivative of formula (5); 3) a step of amidating the optically active beta-amino acid derivative (5) above obtained in 2) to produce an amide of formula (6); 4) a step of alkoxycarbonylating the amide of formula (6) above obtained in 3) to produce a compound of formula (7); and 5) a step of subjecting the compound of formula (7) above to cyclization to produce the optically active tetrahydroquinoline of formula (1).