| 摘要 |
Prepn. of indole derivs. of formula (I) in a single step comprises contacting an N-protected indoline (II) with H2 or hydrogen donor in presence of hydrogenation catalyst with stirring in a solvent at pH at most 7 and at a temp. between ambient and reflux. In (II), R1 is 2-10C alkenyl or benzyl (both opt. substd.); R2-R4 are H, halo (such as Br, Cl, F or I), 1-7C alkyl, aryl, OH, 1-7C alkoxy, 3-7C alkenyloxy, aryloxy, acyloxy, CHO, aroyl, CH2OH, arylhydroxymethyl, COOH, 2-8C alkoxycarbonyl, carbamoyl, amino, mono- or di(1-7C alkyl) amino, 2-8C alkoxycarbonylamino, acylamino, N-(1-7C alkyl) acylamino, di(1-7C alkyl) formamidino or di(1-7C alkoxy) methyl. |
