| abstract |
Prepn. of 3-(alkylamino-methyl)-indole derivs. of formula (I) comprises acid-catalysed reaction of an indole deriv. of formula (II) with an imine of formula R4CH=NR1 (III), in the presence of a prim. amine. In the formulae, R1 = 1-4C alkyl; R4 = 1-4C alkyl or 1-4C alkoxy-(1-2C)-alkyl; R5 = OR6 or CHR7R8; R6 = 1-4C alkyl, 3-6C cycloalkyl or opt. substd. aralkyl; R7 = H or 1-4C alkyl; R8 = H, 1-4C alkyl, OR9 or NR10R11; R9 = 1-4C alkyl; R10, R11 = H or 1-4C alkyl; or R10, R11 = 5-6 membered satd. heterocycle opt. contg. a second heteroatom. |