| 摘要 |
<p>PURPOSE:The introduction of an arbitrary amino group in the 4-position of the indole ring is effected by reaction of 4-oxo-4,5,6,7-tetrahydroindole, the starting material, with an amine to facilitate the production of the titled compound used as a synthetic intermediate of agricultural chemicals and medicines. CONSTITUTION:The reaction of 4-oxo-4,5,6,7-tetrahydroindole of formula I (R<1> is amino-protecting group; X is halogen, H; Y is lalogen) with an amine of formula II (R<2>, R<3> are H, alkyl, aralkyl, alkenyl, aryl, hydroxyl, alkoxy, amino and both groups may incorporate to form a ring) is carried out in a solvent such as tetrahydrofuran, preferably in the presence of sulfuric acid or an organic acid such as sulfonic acid at 50-200 deg.C to give a compound of formula III. The compound of formula I is readily obtained from an N-substituted-4-oxo-4,5,6,7-tetrahydroindole and a halide.</p> |
