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Process Development of a Large-Scale Synthesis of TKA731: A Tachykinin Receptor Antagonist

✍ Scribed by Prashad, Mahavir; Har, Denis; Hu, Bin; Kim, Hong-Yong; Girgis, Michael J.; Chaudhary, Apurva; Repič, Oljan; Blacklock, Thomas J.; Marterer, Wolfgang


Book ID
121080339
Publisher
American Chemical Society
Year
2004
Tongue
English
Weight
171 KB
Volume
8
Category
Article
ISSN
1083-6160

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✍ Lukin, Kirill; Hsu, Margaret C.; Chambournier, Gilles; Kotecki, Brian; Venkatram 📂 Article 📅 2007 🏛 American Chemical Society 🌐 English ⚖ 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