Synthesis of the Selective Serotonin 2A Receptor Agonist 25CN-NBOH
An Improved, Scalable Synthesis of the Selective Serotonin 2A Receptor Agonist 25CN-NBOH: E. Märcher-Rørsted, J. Nykodemová, J. L. Kristensen
SynOpen 2021, 5, 158–160
Psychedelic compounds such as psilocybin and LSD have agonist activity at the serotonin (5-hydroxytryptamine) 2A receptor (5-HT2AR). These psychedelics are also considered putative therapeutics in drug-assisted psychotherapy. Compound 25CN-NBOH (discovered in 2014) has high binding affinity for 5-HT2AR (Ki ~ 1 nM) and is one of the most selective 5-HT2AR agonists reported to date. The group of Professor Jesper L. Kristensen from the University of Copenhagen (Denmark) has recently developed a novel scalable and high-yielding synthetic approach to the title compound, starting from commercially available 2,5-dimethoxyphenethylamine.
Corresponding author Professor Kristensen said: “A novel and facile synthetic route to the selective 5-HT2AR agonist tool compound, 25CN-NBOH, will help make this valuable compound assessable to researchers that seek to understand the serotonin system and the 2A receptor in particular.”