| 摘要 |
A process for producing saxagliptin of formula I that comprises a reaction of the intermediate of formula II, where Boc is tert-butyloxycarbonyl, with a silylating agent in the presence of a base, preferably pyridine, and the intermediate obtained this way is further dehydrated by means of phosphorus oxychloride in the presence of imidazole, producing Boc-saxagliptin of formula IV, which is converted to saxagliptin of formula I by deprotection in an acidic environment, a silylating agent which introduces the trimethyl silyl group being used. |
