| 摘要 |
PURPOSE:To obtain the title compound by catalytic hydrogen reduction of a mineral acid salt of a 1-alkylamino-3-aryloxy-2-propanone using a specific phosphinopyrrolidine compound as ligand for a metal complex compound to be used as catalyst. CONSTITUTION:The objective optically active compound of formula IV (* is asymmetric carbon) can be obtained by catalytic hydrogen reduction of a mineral acid salt of a 1-alkylamino-3-aryloxy-2-propanone of formula I (Ar is carbon ring or heterocycle; R<1> and R<2> are each H, alkyl or benzyl) using, as ligand for a metal complex compound as catalyst, a phosphinopyrrolidine compound of formula II or III [R<3> is H, COR', COOR'', CONHR''', SO2R<4>' or PO(R<5>')2 (R'-R<5>' are each alkyl or aryl); R4 is phenyl; R5 is substituted phenyl]. The present method is excellent in terms of both purity and yield, short in process, thus being advantageous. |
