abstract |
The invention relates to an intermediate of sitagliptin, a preparation method thereof, and an application of the intermediate in the preparation of sitagliptin. The present invention utilizes cheap and easy-to-get epichlorohydrin as a raw material to synthesize intermediate (S)-(2,4,5-trifluorophenyl)epoxypropane and (S)-3-hydroxyl-4-( 2,4,5-trifluorophenyl)butyronitrile introduces a chiral center, avoids the use of various complex chiral reagents, and avoids chiral asymmetric catalytic hydrogenation reactions. It has simple synthetic routes, environmental friendliness and raw materials Low cost and other advantages. |