A scalable synthesis of an azabicyclooctanyl derivative, a novel DPP-4 inhibitor |
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| Authors: | Fei Zhongbo Wu Quanbing Zhang Fei Cao Yudong Liu Chuanqin Shieh Wen-Chung Xue Song McKenna Joe Prasad Kapa Prashad Mahavir Baeschlin Daniel Namoto Kenji |
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| Institution: | Chemical and Analytical Development, Suzhou Novartis Pharma Technology Co. Ltd, Changshu, Jiangsu, China 215537. |
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| Abstract: | A practical synthetic strategy to a chiral azabicycclooctanyl derivative (1), a potent DPP-4 inhibitor, starting from a commercially available nortropine is described. The stereogenic center of 1 was established employing a modified protocol of Ellman's diastereoselective addition of a benzylic nucleophile to tert-butanesulfinimine. Other key steps include Corey-Chaykovsky reaction, Meinwald rearrangement, and CDMT-promoted amide bond formation involving a sterically hindered amine 2. |
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