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Efficient stereocontrolled synthesis of sitagliptin phosphate

Tetrahedron: Asymmetry, 2014
Abstract The synthesis of sitagliptin phosphate 1 , a novel DPP-IV inhibitor for the treatment of type 2 diabetes mellitus has been accomplished starting from the chiral synthon (1,4-bis[( R )-1-phenylethyl]piperazine-2,5-dione) 2 , involving highly stereocontrolled (>98%) alkylation as a key step, in a good overall yield of 50% over six steps.
Chennam Setty Subbaiah, Wahajul Haq
openaire   +1 more source

Pharmacokinetics and relative bioavailability of sitagliptin hydrochloride and sitagliptin phosphate tablets formulations: a randomized, open-label, crossover study in healthy male volunteers

Generics and Biosimilars Initiative Journal, 2023
Introduction/Study Objectives: The present study aimed to evaluate the comparative bioavailability of a new generic sitagliptin formulation. Methods: This was an open label, randomized, balanced, two-sequence, two-treatment, two-period, single oral dose, crossover, bioequivalence (BE) study in 30 healthy male volunteers under fasting conditions.
Chuei Wuei Leong   +9 more
openaire   +1 more source

Sitagliptin Phosphate Monohydrate

2011
Biological target: Sitagliptin is a β-amino acid-derived inhibitor of dipeptidyl peptidase 4 (DPP4), a serine protease with membrane cell-signalling and soluble N-terminal proline peptidase activity. As a result, sitagliptin inhibits the in vivo degradation of the incretins, such as glucagon-like peptide-1 (GLP-1), which are endogenous glucoregulatory ...
Vitomir Šunjić, Michael J. Parnham
openaire   +1 more source

Synthesis of Sitagliptin Phosphate by a NaBH4/ZnCl2-catalyzed Diastereoselective Reduction

Chemistry Letters, 2015
Abstract 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
openaire   +1 more source

Quality by Design Based Analytical Method Development and Validation of Sitagliptin Phosphate by RP-HPLC

International Journal of Research in Pharmacy and Allied Science
The proposed RP- HPLC method using QbD approach provides simple accurate, and reproducible quality analysis for determination of Sitagliptin phosphate. 32 factorial design were used. study interaction of 2 factors were selected as dependent variables i.e mobile phase composition and flow rate and independent variables i.e retention time and tailing ...
Syed Aslam Hamid   +4 more
openaire   +1 more source

FORMULATION AND EVALUATION OF IMMEDIATE RELEASE TABLETS OF SITAGLIPTIN PHOSPHATE

To optimize the clinical management of type 2 diabetes mellitus, this study focuses on the design, development, and comprehensive evaluation of immediate-release Sitagliptin oral tablets using diverse functional excipients and comparative manufacturing techniques.
openaire   +1 more source

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