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

✍ Scribed by Mukund K Gurjar; A.M.S Murugaiah; P Radhakrishna; C.V Ramana; Mukund S Chorghade

• Publisher: Elsevier Science
• Year: 2003
• Tongue: English
• Weight: 283 KB
• Volume: 14
• Category: Article
• ISSN: 0957-4166
• DOI: 10.1016/s0957-4166(03)00157-5

✦ Synopsis

A practical gram scale asymmetric synthesis of CMI-977 is described. A tandem double elimination of an a-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.