762240-92-6Relevant articles and documents
Preparation method of sitagliptin intermediate
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Paragraph 0024; 0030; 0034-0035; 0039-0040; 0044-0045; 0049, (2021/02/13)
The invention relates to a preparation method of a sitagliptin intermediate, and belongs to the technical field of drug intermediate synthesis. In order to solve the problems of low product yield andpoor environmental protection property in the prior art, the invention provides a preparation method of a sitagliptin intermediate, and the method comprises the following steps: reacting 2-piperazinone with hydrazine hydrate in an alcohol solvent to generate piperazine hydrazone; in an acetonitrile or ether solvent, reacting the piperazine hydrazone with ethyl trifluoroacetate to obtain a corresponding intermediate N -[(2Z-) piperazine -2-subunit] trifluoroacethydrazide; and performing cyclization and salification reaction on the N -[(2Z-) piperazine -2-subunit] trifluoroacethydrazide in an alcohol solvent under the action of hydrochloric acid to obtain the corresponding sitagliptin intermediate 3-trifluoromethyl 5, 6, 7, 8-tetrahydro-1, 2, 4-triazole [4, 3-a] pyrazine hydrochloride. The reaction has the effects of high selectivity and high product yield.
Preparation method of sitagliptin intermediate
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Paragraph 0074-0076, (2021/06/22)
The invention discloses a preparation method of a sitagliptin intermediate. The preparation method of the sitagliptin intermediate comprises the following step: in a solvent, carrying out a reaction as shown in the specification on a compound as shown in a formula 2 and a compound as shown in a formula 3 to obtain a compound as shown in a formula 4. The preparation method is high in yield, avoids the use of explosive reagents and phosphorus oxychloride, and is suitable for industrial production.
Design, synthesis, biological evaluation and computational study of novel triazolo [4,3-a]pyrazin analogues
Jethava, Divya J.,Acharya, Prachi T.,Vasava, Mahesh S.,Bhoi, Manoj N.,Bhavsar, Zeel A.,Rathwa, Sanjay K.,Rajani, Dhanji P.,Patel, Hitesh D.
, p. 168 - 192 (2019/03/04)
The triazolo [4,3-a]pyrazin analogues are of interest due to their potential activity against various infectious and non-infectious disease. In search of suitable potent drug candidate, we report here the design, synthesis, characterization, biological activities and computation study of novel triazolo [4,3-a]pyrazin analogues. The synthesized molecules were characterized by various spectroscopic studies such as IR, Mass, 1H NMR, 13C NMR and elemental analysis. The newly synthesized compounds were evaluated for their in vitro biological activities such as anti-malarial, anti-tuberculosis, anti-bacterial and anti-fungal activities against plasmodium falciparum, H37Rv, various bacterial and fungal strains, respectively. The molecular docking study was carried out with enzyme aspartic proteinase zymogen proplasmepsin II from plasmodium falciparum to analyze their binding orientation in the active site of the aspartic proteinase enzyme. The best docking complex was subjected to molecular dynamics simulation to illustrate the stability of these complexes and the most prominent interactions during the simulated trajectory. We have also calculated ADMET properties of all the synthesized compounds to predict the pharmacokinetic properties for the selection of the active and bioavailability of compounds.