Preparation of saxagliptin, a novel DPP-IV inhibitor
…, GS Jones, S Kolotuchin, SA Ramrattan…
Index: Savage, Scott A.; Jones, Gregory S.; Kolotuchin, Sergei; Ramrattan, Shelly Ann; Vu, Truc; Waltermire, Robert E. Organic Process Research and Development, 2009 , vol. 13, # 6 p. 1169 - 1176
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Citation Number: 41
Abstract
The commercial-scale synthesis of the DPP-IV inhibitor, saxagliptin (1), is described from the two unnatural amino acid derivatives 2 and 3. After the deprotection of 3, the core of 1 is formed by the amide coupling of amino acid 2 and methanoprolinamide 4. Subsequent dehydration of the primary amide and deprotection of the amine affords saxagliptin, 1. While acid salts of saxagliptin have proven to be stable in solution, synthesis of the desired free ...
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