PURPOSE: To obtain an optically active compd. useful as an intermediate, such as sterilizer, by an asymmetrical-hydrogenation reaction in an extremely high optical yield by using a catalyst having high activity and enantioselectivity in decreasing the amt. of the catalysts and shortening the reaction time.
CONSTITUTION: The optically active compd. of formula V is advantageously obtd. by subjecting the compd. formula I (R1 is H, formula II; R2 is methyl, ethyl, chloromethyl; R3 is a 1 to 4C alkyl, R2 and R3 are each a 3 to 7C cycloalkyl together with C to which both are bonded) to the asymmetric hydrogenation at a temp. of about 20 to 140°C, more preferably about a temp. of 80 to 120°C in the presence of the neutral or cationic rhodium complex of preferably a chiral atropisomerism phosphine, more particularly the rhodium catalysts of formula III or formula IV (X is coordination anionic ligand; Y is chiral atropisomerism diphosphine ligand; L is neutral ligand; A is anion). The compd. may be converted to the compd. of formula VI (R1 is Z; NR is N-piperidinyl, etc.) by a known method.
IBUO KURAMERI
HANSU PEETAA IIZENRINKU
ARUBERUTO PUFUITSUFUNAA
