An improved synthesis of cis-4-phenyl-2-propionamidotetralin (4-P-PDOT): a selective MT(2) melatonin receptor antagonist |
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Authors: | Lucarini Simone Bedini Annalida Spadoni Gilberto Piersanti Giovanni |
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Institution: | Institute of Medicinal Chemistry, University of Urbino "Carlo Bo", Piazza del Rinascimento 6, 61029 Urbino (PU), Italy. |
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Abstract: | A novel, efficient and diastereoselective procedure was developed for the gram-scale synthesis of cis-4-phenyl-2-propionamidotetralin (4-P-PDOT), a selective MT(2) melatonin receptor antagonist. The synthetic strategy involved the conversion of 4-phenyl-2-tetralone to enamide followed by diastereoselective reduction affording cis-4-P-PDOT in good yield. The mechanism of the reduction step was explored by employing deuterated reagents. |
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