Wang En-jun
2011
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Journal
Strait Pharmaceutical Journal
Abstract
OBJECTIVE To synthesize Alogliptin benzoate.METHODS Alogliptin benzoate was synthesized from 6-chloro-3-methyluracil and 2-(bromomethyl)benzonitrile by alkylation to give 2-(6-chloro-3-methyl-2,4-dioxo-3,4-di-hydro-2H-pyrimidin-1-ylmethyl)benzonitrile,which was subjected to displacement with 3(R)-aminopiperidine in the presence of alkali and salt formation.RESULTS and CONCLUSION The structure of Alogliptin benzoate was confirmed by 1H-NMR,and MS.The process is suitable for industrial preparation and more practical owing to its advantages of low cost,convenient operations and good yield of 56.1%.