Synthesis of two isotopically labeled 5-HT1B antagonists

摘要

Serotonin (5-HT) is a neurotransmitter, and dysfunctions of its transmission have been implicated in a large number of disease states including migraines, anxiety, depression, and obesity.1 5-HT1B antagonists have been suggested as potential treatments for depression and anxiety and have been shown to be effective in animal models of these disease states.2 During development of 5-HT1B antagonists, C-14 labeled AR-A000002 and tritium labeled M-549865 were required and their syntheses will be discussed herein.