| 摘要 |
PURPOSE:To produce the desired optically active compound useful as an important intermediate for medicines from an optically active 3-chloro-2-propanol derivative having relatively high reactivity without lowering the optical purity. CONSTITUTION:A compound of formula I (R<1> is 2.2-diphenylacetyl, diphenylmethyl, 5-dibenzsuberanyl; 1c is asymmetric carbon) is treated with a base in a proper solvent under ice cooling or at room temperature, and subsequently reacted with an aromatic hydroxy compound or a heterocyclic ring hydroxy compound in the presence of a base to produce an optically active 2-propanol derivative of formula II (R<2> is phenyl, naphthyl or heteroaromatic ring which is not substituted or is substituted with lower alkyl, lower alkoxy, halogen, CN, or NO2). The compound of formula III (R<2> is quinoline ring) among the compound of formula II is useful as a carcinostatic effect-augmenting agent. The compound of formula I is easily obtained from optically active epichlorohydrin and a piperidine derivative. |
