Title of article :
Efficient synthesis of sitagliptin phosphate, a novel DPP-IV inhibitor, via a chiral aziridine intermediate
Author/Authors :
Pan، نويسنده , , Xianhua and Li، نويسنده , , Xiaojun and Lu، نويسنده , , Qingling and Yu، نويسنده , , Wansheng and Li، نويسنده , , Weijin and Zhang، نويسنده , , Qunhui and Deng، نويسنده , , Fei and Liu، نويسنده , , Feng، نويسنده ,
Issue Information :
هفته نامه با شماره پیاپی سال 2013
Abstract :
Sitagliptin phosphate, a novel DPP-IV inhibitor of T2DM, has been synthesized via 12 linear steps, in an overall yield of 26%. The key step is the coupling reaction of 2,4,5-trifluorophenylmagnesium bromide with a chiral aziridine derivative, which was prepared from l-homo-serine by simple steps.
Keywords :
Synthesis , Sitagliptin phosphate , ?-Amino acid , Grignard reaction , aziridine
Journal title :
Tetrahedron Letters
Journal title :
Tetrahedron Letters
