Efficient synthesis of sitagliptin phosphate, a novel DPP-IV inhibitor, via a chiral aziridine intermediate

Autor:	Xianhua Pan, Deng Fei, Wansheng Yu, Weijin Li, Qingling Lu, Qunhui Zhang, Li Xiaojun, Feng Liu
Rok vydání:	2013
Předmět:	chemistry.chemical_compound chemistry Bromide Stereochemistry Yield (chemistry) Organic Chemistry Drug Discovery Grignard reaction Aziridine Biochemistry Coupling reaction Derivative (chemistry) Sitagliptin Phosphate
Zdroj:	Tetrahedron Letters. 54:6807-6809
ISSN:	0040-4039
DOI:	10.1016/j.tetlet.2013.09.136
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::c22a46389c8e8d75565a0e649622232e https://doi.org/10.1016/j.tetlet.2013.09.136 Zobrazit plný text záznamu Full Text from ScienceDirect