Name: Omarigliptin
CAS#: 1226781-44-7
Chemical Formula: C17H20F2N4O3S
Exact Mass: 398.12242
Molecular Weight: 398.43
Elemental Analysis: C, 51.25; H, 5.06; F, 9.54; N, 14.06; O, 12.05; S, 8.05
EOS Med Chem produce Omarigliptin MK3102 1226781-44-7 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Omarigliptin MK3102 1226781-44-7 Intermediates, EOS Med Chem have 8; Omarigliptin MK3102 1226781-44-7 Impurity we have 10, all from GMP, FDA plant.
Now Omarigliptin MK3102 1226781-44-7 DMF document is preparing.
Until 2016, Aug, Omarigliptin MK3102 1226781-44-7 more than produced 25kg API, 120kg Intermediates
omarigliptin Intermediate N-[(2R,3S)-2-(2,5-difluorophenyl)tetrahydro-5-oxo-2H-pyran-3-yl]-CarbaMic acid 1,1-diMethylethyl ester 951127-25-6
omarigliptin Intermediate 2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole 1280210-80-1
Description: Omarigliptin, also known as MK-3102, is a potent and long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. MK-3102 (omarigliptin), was identified as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor with an excellent pharmacokinetic profile amenable for once-weekly human dosing and selected as a clinical development candidate. Omarigliptin is currently in phase 3 clinical development.
Synonym: MK3102; MK-3102; MK 3102; Omarigliptin
IUPAC/Chemical Name: (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine
SMILES Code: N[C@@H]1[C@@H](C2=CC(F)=CC=C2F)OC[C@H](N3CC4=NN(S(=O)(C)=O)C=C4C3)C1
1: Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014 Apr 24;57(8):3205-12. doi: 10.1021/jm401992e. Epub 2014 Apr 2. PubMed PMID: 24660890.
2: Biftu T, Qian X, Chen P, Feng D, Scapin G, Gao YD, Cox J, Roy RS, Eiermann G, He H, Lyons K, Salituro G, Patel S, Petrov A, Xu F, Xu SS, Zhang B, Caldwell C, Wu JK, Lyons K, Weber AE. Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2- (2,5-difluorophenyl)-5-(4,6-dihydropyrrolo [3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23) [corrected]. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5361-6. doi: 10.1016/j.bmcl.2013.07.061. Epub 2013 Aug 5. Erratum in: Bioorg Med Chem Lett. 2014 Jun 1;24(11):2590. PubMed PMID: 23972441.
