ChemInform Abstract: Lactones. Part 24. “γ‐Lactonized” Neuroleptics. Synthesis, Stereochemistry, and Affinity at the D2 Receptor.

Abstract

Lactones. Part 24. "γ-Lactonized" Neuroleptics. Synthesis, Stereochemistry, and Affinity at the D2 Receptor.-Carboxylation of the lactone (I) produces the carboxylic acid (III) which is converted to the methylene lactone (V) by Mannich reaction, decarboxylation, and elimination of amine. Addition reaction of the piperidines (VI) to (V) forms the target "γ-lactonized" neuroleptics (VII). Analogously, the 3,4-disubstituted lactones (VIII) are synthesized. The affinity of the neuroleptics (VII) and (VIII) to the D2 receptor in rat brain is investigated. -(LEHMANN, J.; SCHULZE, G.; RADWANSKY, A.; Arch.