| 摘要 |
PURPOSE:To easily obtain the subject compound having (R)-configuration and useful as a production intermediate for a remedy for hypertension, in high yield, efficiency and asymmetric yield, by carrying out asymmetric hydrogenation of a substituted methylenepropionic acid derivative using a specific rhodium complex catalyst. CONSTITUTION:The objective compound of formula II (* represents asymmetric C) having excellent renin-inhibitory activity and useful as a production intermediate for a remedy for hypertension, by carrying out asymmetric hydrogenation of a substituted methylenepropionic acid derivative of formula I (R<1> and R<2> are H, lower alkyl, aralkyl or aryl or -NR<1>R<2> forms a cyclic amino which may contain hetero atom in addition to the bonded N atom) in the presence of a univalent rhodium complex catalyst containing an optically active phosphine as a ligand, e.g., (2R,4R)-N-tert-butoxycarbonyl-4- diphenylphosphino-2-(diphenylphosphinomethyl)pyrrolidine and chloro(1,5- cyclooctadiene)rhodium (I) dimer. |
