N-[(3S)-1-Benzylpyrrolidin-3-yl]-(2-thienyl)benzamides: Human dopamine D4 ligands with high affinity for the 5-HT2A receptor

A series of N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides 8 has been prepared and found to bind with high affinity to the human D4 (hD4) and 5-HT2A receptors. Several compounds displayed selectivity for these receptors versus hD2 and α1 adrenergic receptors of over 500-fold.