SYNTHESIS OF NOVEL 5-(2-(PHENYLSULFONYL)ETHYL)-1H-INDOLE DERIVATIVES

摘要

An objective of the present invention is to develop commercially viable methods for the synthesis of 5-[2-phenylsulfony)ethyl]-1H-indole of Formule (II), where R¹ and R² are same or different and each independently represent a hydrogen, fluorine, or di(lower alkyl)amino, acyl, or alkoxy carbonyl or chlorine atom, or a lower alkyl, lower alkoxy, nitro, cyano, aminolower alkylamine group Formula (II). Another objective of the present invention is to convert the product Formula (II) to Formula (I) in high yields, where R¹ and R² are same or different and each independently represent a hydrogen, fluorine, or di(lower alkyl)amino, acyl, or alkoxy carbonyl or chlorine atom, or a lower alkyl, lower alkoxy, nitro, cyano, aminolower alkylamine group Formula (I). One of the first processes attempted was by reacting the indole derivative of Formula (III) with aryl vinyl sulphones of Formula (V) as shown in Scheme-III. Another process attempted was by reacting the aniline derivative of Formula (VI) with aryl sulphones of Formula (VII) as shown in Scheme-III. Scheme IV.