New calcineurin inhibiting 3-dimethylaminopropyl substituted diarylheterocycles by Sonogashira reactions and catalytic hydrogenation

摘要

A series of calcineurin inhibiting compounds I consisting of a central aromatic N-heterocycle, two aryl substituents and a 3-dimethylaminopropyl chain was synthesized by introduction of the side chain. A corresponding haloheterocycle 3 was transformed into a 3-dimethylaminopropynylheterocycle 2 by Sonogashira coupling and was in turn hydrogenated in the presence of Pd/C to afford the 3 -dimethylaminopropyl-substiuted heterocycles 1. Some of the products showed calcineurin inhibiting activity.