Stereoselective Transaminase‐Mediated Synthesis of Serotonin and Melatonin Receptor Agonists

Transaminase enzymes have significant potential for the stereoselective synthesis of drugs or drug precursors. Here, starting from one prochiral β-tetralone, a short and efficient chemoenzymatic four agonists serotonin/melatonin receptors been developed. The key step is transamination ketone to produce both enantiomers 8-methoxy-2-aminotetraline in high yields enantiomeric excesses. This was followed by either amidation give 8-methoxy-2-acetimidotetralines several facile chemical steps 8-hydroxy-2-aminodipropyltetralines.