摘要 |
<p>PURPOSE:To easily obtain a 1-hydroxyindole by protecting the OH group of a 1-hydroxy-2-oxyindole as a raw material, reducing the reaction product, introducing a prescribed substituent to the reduction product, and finally removing the protecting group through a partially new intermediates. CONSTITUTION:A 1-hydroxy-2-oxyindole of formula I [the ring A is (substituted) benzene] is reacted with a compound of formula: HOCH2CH2-R (R is pyridyl, 2-trialkylsilyl) to obtain a 1-O-substituted oxyindole of formula II in which the OH is protected). The compound is reduced to obtain a 1-O-substituted indole of formula III. A substituent is introduced into the 3-position of the obtained 1-O-substituted indole. The protecting group is finally removed from the obtained compound of formula IV to obtain a 1-hydroxyindole of formula V. The 1-O-substituted-2-oxyindole of formula VI and the 1-O-substituted indole of formula VII are new among the intermediates obtained by the reactions.</p> |