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.

The study demonstrates a method for synthesis of 2,4,5-trifluorophenylacetic acid, the starting material for sitagliptin, using 1,2,4-trifluorobenzene and Pd/C and formic acid, with potential applications in DPP-4 inhibitors.

Paper

Study on synthesis of 2,4,5-trifluorophenylacetic acid

References

Citations