Synthesis of chiral β-methyl tryptamine-derived GnRH antagonists

…, MM Ponpipom, MT Goulet, MS Levorse, RC Desai

Index: Simeone, Joseph P.; Bugianesi, Robert L.; Ponpipom, Mitree M.; Goulet, Mark T.; Levorse, Mark S.; Desai, Ranjit C. Tetrahedron Letters, 2001 , vol. 42, # 37 p. 6459 - 6461

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Citation Number: 18

Abstract

During the course of our investigation into the development of potent non-peptide gonadotropin releasing hormone antagonists, 1., , and we became interested in the synthesis of 2-aryl-β-methyl tryptamine derivatives. We found that the introduction of a methyl group β to the tryptamine nitrogen provided increased potency and selectivity over the non-substituted analogs, when evaluated in our screening protocol. 2 This discovery prompted us to develop a stereospecific ...