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Halogenation of a capsaicin analogue leads to novel vanilloid TRPV1 receptor antagonists

โœ Scribed by Giovanni Appendino; Selena Harrison; Luciano De Petrocellis; Nives Daddario; Federica Bianchi; Aniello Schiano Moriello; Marcello Trevisani; Francesca Benvenuti; Pierangelo Geppetti; Vincenzo Di Marzo


Book ID
110007920
Publisher
Nature Publishing Group
Year
2003
Tongue
English
Weight
201 KB
Volume
139
Category
Article
ISSN
0007-1188

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โœ Lukin, Kirill; Hsu, Margaret C.; Chambournier, Gilles; Kotecki, Brian; Venkatram ๐Ÿ“‚ Article ๐Ÿ“… 2007 ๐Ÿ› American Chemical Society ๐ŸŒ English โš– 104 KB

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 it