Prepn. of 2- or 13-acyl-ergoline derivs. for pharmaceuticals - by acylation reaction in presence of lewis acid and opt. removing protecting gp.

摘要

Prepn. of 2- or 13-acyl-ergoline derivs. of formula (I) and their salts comprises acylation of an ergoline deriv. of formula (II) in the presence of a Lewis acid and opt. removing the protecting gp. or forming the acid addn. salt. In the formulae, R1 = a protecting gp.; R3 = H, 1-4C alkyl, 6-10C aryl or 7-10C aralkyl; R6 = 1-6C alkyl, 3-6C alkenyl or 3-5C cycloalkyl-(1-2C)alkyl; X = O or S. Acylation takes place in the 13-position when an acid halide is used while the 2-position is acylated when a dichloromethylalkyl ether is used. USE/ADVANTAGE - (I) are active pharmaceutical agents and intermediates in the prepn. of other ergoline derivs. The process involves few steps, is regioselective, does not require costly and difficult sepn. operations, and gives good yields of (I).