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2017年1月6日星期五

GMP: Omarigliptin, MK-3102, 1226781-44-7

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

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
We produce Omarigliptin, MK-3102, 1226781-44-7 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Omarigliptin, MK-3102, 1226781-44-7 Intermediates, we have 8; Omarigliptin, MK-3102, 1226781-44-7 Impurity we have 10, all from GMP, FDA plant.

Now Omarigliptin, MK-3102, 1226781-44-7 DMF document is preparing.

Until 2016, Aug, Omarigliptin, MK-3102, 1226781-44-7 more than produced 25kg API, 120kg Intermediates
Omarigliptin MK-3102;Marizev 1226781-44-7
Omarigliptin Intermediates (2S,3R,5S)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine 1443380-88-8
Omarigliptin Intermediates Tert-butyl 4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate 1280210-79-8
Omarigliptin Intermediates 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole 4-methylbenzenesulfonate 18193664-02-7
Omarigliptin Intermediates Tert-butyl 2-(methylsulfonyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate 1226781-82-3
Omarigliptin Intermediates (Z)-tert-butyl 3-((dimethylamino)methylene)-4-oxopyrrolidine-1-carboxylate 905274-02-4
Omarigliptin Intermediates Tert-butyl 6a-hydroxy-1,2,6,6a-tetrahydropyrrolo[3,4-c]pyrazole-5(4H)-carboxylate 1211594-55-6
Omarigliptin Intermediates 2-(methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole 1226781-80-1
Omarigliptin Intermediates 2-(methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole benzenesulfonate 1280210-80-1
Omarigliptin Intermediates Tert-butyl ((2R,3R)-2-(2,5-difluorophenyl)-5-oxotetrahydro-2H-pyran-3-yl)carbamate 1456616-43-5
Omarigliptin Intermediates Tert-butyl ((2S,3S)-2-(2,5-difluorophenyl)-5-oxotetrahydro-2H-pyran-3-yl)carbamate 1456616-44-6
Omarigliptin Intermediates (2R,3R,5R)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine
Omarigliptin Intermediates (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(pyrrolo[3,4-c]pyrazol-5(1H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine
Omarigliptin Intermediates Tert-butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl)carbamate 1172623-99-2
Omarigliptin Intermediates 2-((tert-butoxycarbonyl)amino)pent-4-ynoic acid 61172-66-5
Omarigliptin Intermediates Tert-butyl (1-(methoxy(methyl)amino)-1-oxopent-4-yn-2-yl)carbamate 172623-95-8
Omarigliptin Intermediates Tert-butyl (1-(2,5-difluorophenyl)-1-oxopent-4-yn-2-yl)carbamate 1172623-96-9
Omarigliptin Intermediates (2R,3S,5R)-2-(3-fluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine
impurity A
Omarigliptin Intermediates (2R,3S,5R)-2-(2-fluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine impurity B