764667-65-4Relevant articles and documents
Preparation method of sitagliptin phosphate intermediate
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Paragraph 0030-0031; 0038-0043, (2021/11/21)
The invention discloses a preparation method of a sitagliptin phosphate intermediate. In the existing synthesis method of the sitagliptin phosphate intermediate, a corresponding post-treatment method is not reported or the reported post-treatment method is tedious in operation, low in solvent recovery rate, capable of generating a large amount of three wastes, and not beneficial to environmental protection. The method comprises the following steps: directly evaporating to remove a solvent after the synthesis reaction of the sitagliptin phosphate intermediate is completed, adding a crystallization solvent, cooling, stirring for crystallization, washing and drying to obtain the corresponding sitagliptin phosphate intermediate. According to the invention, the yield and the purity of the sitagliptin phosphate intermediate are improved; the method is simple in process, high in solvent recovery rate and suitable for large-scale industrial production, and wastewater is not generated in the production process.
Sitagliptin impurity as well as removal method and application thereof
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Paragraph 0046-0050, (2021/07/17)
The invention provides a sitagliptin impurity as well as a removal method and an application of the sitagliptin impurity, and particularly discloses an impurity in the production of a sitagliptin intermediate 4-oxo-4-[3-(trifluoromethyl)-5, 6-dihydro-[1, 2, 4] triazolo [4, 3-a] pyrazine-7-(8H)-yl]-1-(2, 4, 5-trifluorophenyl) butyl-2-ketone, and through the discovery of the impurity, the quality standard of sitagliptin or sitagliptin phosphate hydrate can be remarkably improved.
NEW EFFICIENT PROCESS FOR THE PREPARATION OF SITAGLIPTIN.
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, (2019/09/06)
Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine. (I)