[Indoles. 10. Synthesis, structure and D2-affinity of beta-carboline analogs of flutroline]

Abstract

10 is a beta-carboline analogue of the neuroleptic flutroline2a,b) with significant lower affinity at the dopamine D2 binding site. Various synthetic routes to 10 and the solid state structure of 8 are described, structure activity relations, in particular the importance of the "S-shape" and the rigid dopamine conformation are discussed.