Liu Ze-ling
2011
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Journal
Hebei Journal of Industrial Science and Technology
Abstract
The preparation of 2,4,5-trifluorophenylacetic acid,which is the starting material of sitagliptin,the first DPP-4 inhibitors,is achieved,with 1,2,4-trifluorobenzene as materials,through Friedel-Crafts acylation,hydrolysis rearrangement in base environment,chlorination and hydrogenolysis catalyzed by Pd/C and formic acid.The effect of the catalyst and temperature were investigated.