Sitagliptin
Title: Sitagliptin
CAS Registry Number: 486460-32-6
CAS Name: 7-[(3R)-3-Amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine
Additional Names: (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Molecular Formula: C16H15F6N5O
Molecular Weight: 407.31
Percent Composition: C 47.18%, H 3.71%, F 27.99%, N 17.19%, O 3.93%
Literature References: Selective inhibitor of dipeptidyl peptidase IV (DPP-IV). Prepn: S. D. Edmondson et al., WO 03004498; eidem, US 6699871 (2003, 2004 both to Merck & Co.); and enzyme inhibitory profile: D. Kim et al., J. Med. Chem. 48, 141 (2005). Improved process: K. B. Hansen et al., Org. Process Res. Dev. 9, 634 (2005). Clinical pharmacokinetics and pharmacodynamics: G. A. Herman et al., Clin. Pharmacol. Ther. 78, 675 (2005). Review: C. F. Deacon, Curr. Opin. Invest. Drugs 6, 419-426 (2005).
Properties: Viscous oil.
 
Derivative Type: Monophosphate monohydrate
CAS Registry Number: 654671-77-9; 654671-78-0 (anhydrous)
Additional Names: Sitagliptin phosphate
Manufacturers' Codes: MK-0431
Trademarks: Januvia (Merck & Co.)
Molecular Formula: C16H15F6N5O.H3PO4.H2O
Molecular Weight: 523.32
Percent Composition: C 36.72%, H 3.85%, F 21.78%, N 13.38%, O 18.34%, P 5.92%
Properties: mp 215-217°. [a]D -74.4° (c = 1.0 in water).
Melting point: mp 215-217°
Optical Rotation: [a]D -74.4° (c = 1.0 in water)
 
Therap-Cat: Antidiabetic.
Keywords: Antidiabetic; Dipeptidyl Peptidase IV Inhibitors .

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