Highly enantioselective synthesis of sitagliptin
| Title | Highly enantioselective synthesis of sitagliptin |
| Publication Type | Journal Article |
| Year of Publication | 2020 |
| Authors | V. Khopade, K, Sen, A, Birajdar, RS, Paulbudhe, UP, Kavale, DS, Shinde, PS, Mhaske, SB, Chikkali, SH |
| Journal | Asian Journal of Organic Chemistry |
| Volume | 9 |
| Issue | 2 |
| Pagination | 189-191 |
| Date Published | FEB |
| Type of Article | Article |
| ISSN | 2193-5807 |
| Keywords | asymmetric hydrogenation, catalysis, FerroLANE ligands, Rhodium, sitagliptin |
| Abstract | 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. |
| DOI | 10.1002/ajoc.201900709, Early Access Date = JAN 2020 |
| Type of Journal (Indian or Foreign) | Foreign |
| Impact Factor (IF) | 3.130 |
Divison category:
Organic Chemistry
Polymer Science & Engineering