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Synthesis of Sitagliptin Phosphate by a NaBH4/ZnCl2-catalyzed Diastereoselective Reduction
Chemistry Letters, 2015Abstract A practical asymmetric synthesis of sitagliptin phosphate, from 1-{3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo-[4,3-a]pyrazin-7(8H)-yl}-4-(2,4,5-trifluorophenyl)butane-1,3-dione, in overall 65.3% yield has been reported. The target compound was synthesized via eneamination, diastereoselective reduction, amine-deprotection ...
Xianhua Pan +5 more
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Chemistry - An Asian Journal, 2020
An alternate formal synthesis of Sitagliptin phosphate is disclosed from 2,4,5-trifluorobenzadehyde in 8 linear steps with an overall yield of 31.16%.
Kurella Sreenivasulu +7 more
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An alternate formal synthesis of Sitagliptin phosphate is disclosed from 2,4,5-trifluorobenzadehyde in 8 linear steps with an overall yield of 31.16%.
Kurella Sreenivasulu +7 more
semanticscholar +1 more source
Sitagliptin phosphate: A DPP-4 inhibitor for the treatment of type 2 diabetes mellitus
Clinical Therapeutics, 2007Sitagliptin phosphate, the first dipeptidyl peptidase 4 (DPP-4) inhibitor, provides a new treatment option for patients with type 2 diabetes.The purpose of this article is to review the pharmacology, pharmacokinetics, pharmacodynamics, clinical efficacy, adverse effects, and cost of sitagliptin in adults with type 2 diabetes.A literature search of ...
Tina, Zerilli, Eunice Y, Pyon
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Tetrahedron Letters, 2013
Sitagliptin phosphate, a novel DPP-IV inhibitor of T2DM, has been synthesized via 12 linear steps, in an overall yield of 26%. The key step is the coupling reaction of 2,4,5-trifluorophenylmagnesium bromide with a chiral aziridine derivative, which was prepared from l-homo-serine by simple steps.
Xianhua Pan +7 more
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Sitagliptin phosphate, a novel DPP-IV inhibitor of T2DM, has been synthesized via 12 linear steps, in an overall yield of 26%. The key step is the coupling reaction of 2,4,5-trifluorophenylmagnesium bromide with a chiral aziridine derivative, which was prepared from l-homo-serine by simple steps.
Xianhua Pan +7 more
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Journal of Thermal Analysis and Calorimetry, 2023
Rajkumar Malayandi +5 more
semanticscholar +1 more source
Rajkumar Malayandi +5 more
semanticscholar +1 more source
2023
Abstract The aim of this research work was to formulate fast-dissolving oral films of sitagliptin phosphate for the treatment of diabetes mellitus. The fast dissolving films of sitagliptin phosphate were prepared by solvent casting method using film forming polymers HPMC E 15 and HPMC E 50 cps and PEG and propylene glycol are used as plasticizers. All
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Abstract The aim of this research work was to formulate fast-dissolving oral films of sitagliptin phosphate for the treatment of diabetes mellitus. The fast dissolving films of sitagliptin phosphate were prepared by solvent casting method using film forming polymers HPMC E 15 and HPMC E 50 cps and PEG and propylene glycol are used as plasticizers. All
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Case of lichen planus induced by sitagliptin phosphate hydrate
The Journal of Dermatology, 2016Akiko Ohtani +3 more
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