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Highly Enantioselective Synthesis of Sitagliptin
Asian Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2020-01-17 , DOI: 10.1002/ajoc.201900709 Kishor V. Khopade 1 , Anirban Sen 1, 2 , Rajkumar S. Birajdar 1, 2 , Uday P. Paulbudhe 1 , Dattatry S. Kavale 3 , Prashant S. Shinde 3 , Santosh B. Mhaske 3 , Samir H. Chikkali 1, 2
Asian Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2020-01-17 , DOI: 10.1002/ajoc.201900709 Kishor V. Khopade 1 , Anirban Sen 1, 2 , Rajkumar S. Birajdar 1, 2 , Uday P. Paulbudhe 1 , Dattatry S. Kavale 3 , Prashant S. Shinde 3 , Santosh B. Mhaske 3 , Samir H. Chikkali 1, 2
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A highly enantioselective synthesis of sitagliptin, a potent DPP‐4 inhibitor, is reported. Explicitly identified chiral FerroLANE ligands in the presence of rhodium catalyze the asymmetric hydrogenation of an enamine to yield sitagliptin with excellent enantioselectivity (98% ee). The process was scaled up to 5 g and the final product was isolated as a phosphate salt with >99% ee.
中文翻译：
西他列汀的高度对映选择性合成
据报道西他列汀是一种强力的DPP-4抑制剂，具有高度对映选择性。在铑的存在下明确鉴定的手性FerroLANE配体催化烯胺的不对称氢化，产生具有出色对映选择性（98％ee）的西他列汀。将该工艺放大至5g，并分离出最终产物，其为具有> 99％ee的磷酸盐。
更新日期：2020-01-17
中文翻译：
西他列汀的高度对映选择性合成
据报道西他列汀是一种强力的DPP-4抑制剂，具有高度对映选择性。在铑的存在下明确鉴定的手性FerroLANE配体催化烯胺的不对称氢化，产生具有出色对映选择性（98％ee）的西他列汀。将该工艺放大至5g，并分离出最终产物，其为具有> 99％ee的磷酸盐。
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