用于治疗2-型糖尿病的含氟药物西格列汀的合成方法与研究进展  

Progress in Synthesis of Fluorine-Containing Drug Sitagliptin for Treating Type 2 Diabetes

作　　者：吕太勇[1] 罗源军[1] 刘波[1] 钟新平[1] 李斌[1] 张建新[1] 

机构地区：[1]中昊晨光化工研究院有限公司,四川自贡643201

出　　处：《有机氟工业》2015年第4期37-41,共5页Organo-Fluorine Industry

摘　　要：氟具有极强的电负性和氧化性,化合物经氟取代后可获得截然不同的化学/立体化学效果。综述了近年来用于治疗2-型糖尿病药物西格列汀的各种合成工艺进展,对其合成工艺的优缺点进行了分析,并对西格列汀新的合成工艺进行了展望。Fluorine possesses some extreme properties,in particular,ultimate electronegativity and oxidation potential. Therefore,substitution of trifluoromethyl for a methyl group or pentafluorophenyl for a phenyl group can lead to a dramatically different chemical / stereochemical outcome. This paper reviews the recent progress of various synthetic routes of sitagliptin for type 2 diabetes treatment. The advantages and disadvantages of those synthetic routes are described,and new synthetic routes are discussed.

关 键 词：含氟药物 西格列汀 合成工艺 进展 

分 类 号：TQ460.1[化学工程—制药化工]