反应详情

A mixture of 5.10 g (0.017 mol) of 4-(5-fluoroindol-3-yl)butyl methanesulfonate [obtainable by reaction of 4-(5-fluoroindol-3-yl)butanol (obtainable by lithium aluminium hydride reduction of 4-(5-fluoroindol-3-yl)butanoic acid, which can be prepared analogously to a Japp-Klingemann reaction, in THF) with methanesulfonyl chloride], 4.0 g (0.015 mol) of 4-(2-oxo-2H-1-benzopyran-6-yl)piperazine, hydrochloride (obtainable as described in Example 1), 200 ml of acetonitrile and 10.0 ml of triethylamine is reacted for 30 hours on a steam bath with stirring. After customary working up, 3-{4-[4-(2-oxo-2H-1-benzopyran-6-yl)-1-piperazinyl]butyl}-5-fluoroindole, hydrochloride, m.p. 293-295°, is obtained.

1. customis reacted for 30 hours on a steam bath