Process for the preparation of (3-cyano-1H-indol-7-yl)(4-(4-fluorophenethyl)piperazin-1-yl)-methanone and salts thereof

摘要

Process for the preparation of (3-cyano-1H-indol-7-yl)[4-(4-fluorophenethyl)piperazin-1-yl]methanone of formula I where: 1) an indole ester of formula II is formylated, where R is an alkyl group having from 1 to 6 carbon atoms or arylalkyl. 2) The formyl ester of formula III is formed from (1) is reacted with hydroxylamine to give an oxime derivative of formula IV, where R is defined above. 3) The oxime of formula IV is converted into a cyanoindole ester of formula V, where R is defined above. 4) The ester of formula V is saponified to give 3-cyano-1H-indole-7-carboxylic acid, and 5) The 3-cyano-1H-indole-7-carboxylic acid is reacted with 1-[2-(4-fluorophenyl)ethyl]piperazine to give the compound of formula I, and 6) The resultant base of formula I is converted into one of its salts by treating with acid.