5-substituted 3,4-dihydro-3-amino-2H-1-benzopyran derivatives: synthesis and interaction with serotoninergic receptors

A new series of 3,4-dihydro-3-amino-2H-1-benzopyran derivatives (1 and 2) b earing various substituents on the 5-position was successfully prepared via palladium-mediated cross-coupling reactions. Some of the new compounds sho wed high affinity for 5-HT1A and 5-HT7 receptors. The best affinity for the 5-HT1A and 5-HT7 receptors was obtained for 2b (K-i = 0.3 nM for 5-HT1A an d 3.1 nM for 5-HT7). The anxiolytic activity of compound 2b was evaluated.