A novel and simple asymmetric synthesis of CMI-977 (LDP-977): a potent anti-asthmatic drug lead

…, P Radhakrishna, CV Ramana, MS Chorghade

Index: Gurjar, Mukund K.; Murugaiah; Radhakrishna; Ramana; Chorghade, Mukund S. Tetrahedron Asymmetry, 2003 , vol. 14, # 10 p. 1363 - 1370

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Citation Number: 29

Abstract

A practical gram scale asymmetric synthesis of CMI-977 is described. A tandem double elimination of an α-chlorooxirane and concomitant intramolecular nucleophilic substitution was used as the key step. Jacobsen hydrolytic kinetic resolution and Sharpless asymmetric epoxidation protocols were applied for the execution of the synthesis of the key chiral building block.