| 摘要 |
Prodn. of optically active 1-aryl-alkylamines of formula (I) comprises: (a) hydrogenating a 2-aryl-propenoic acid of formula (II) in the presence of a chiral transition metal bisphosphine complex, a diluent and opt. a tert. amine; (b) reacting the resulting optically active 2-arylpropionic acid of formula (III) with SOCl2 and then with NH3; and (c) reacting the resulting optically active 2-arylpropionamide of formula (IV) with NaOCl or NaOBr in the presence of water: R<1> = H or alkyl; Ar = phenyl or naphthyl substd. by 0-5 of halo, alkyl, alkoxy, haloalkyl, haloalkoxy, CN, dialkylamino, Ph and/or benzyl. |
