Development of a Large Scale Asymmetric Synthesis of Vanilloid Receptor (TRPV1) Antagonist ABT-102

✍ Scribed by Lukin, Kirill; Hsu, Margaret C.; Chambournier, Gilles; Kotecki, Brian; Venkatramani, C. J.; Leanna, M. Robert

• Book ID: 124057980
• Publisher: American Chemical Society
• Year: 2007
• Tongue: English
• Weight: 104 KB
• Volume: 11
• Category: Article
• ISSN: 1083-6160
• DOI: 10.1021/op060228s

✦ Synopsis

A highly efficient asymmetric synthesis of TRPV1 antagonist ABT-102 was developed and successfully demonstrated on a multi-kilogram scale. This process incorporates a new asymmetric synthesis of (R)-tert-butylaminoindan, which is based on a chiral auxiliary induced diastereoselective reduction of its iminoindan precursor.