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Stereoselective Transaminase-Mediated Synthesis of Serotonin and Melatonin Receptor Agonists

Transaminase enzymes have significant potential for the stereoselective synthesis of drugs or drug precursors. In this Technical Publication, a short and efficient chemoenzymatic synthesis of four agonists of the serotonin/melatonin receptors have been developed. This was followed by either amidation to give the 8-methoxy-2-acetimiditetralines or several facile chemical steps to the 8-hydroxy-2-aminodipropyltetralines.

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