Korea customer site audit me, 100% pass,
All China purity by HPLC/MS analysis is only 91.35%
Should use wavelength of 254 nm. But, the spectrum all china used was obtained at 205 nm.
And the column has been changing to normal phase column from reverse phase column. We could not understand why all china how to load 40 uL at 2 mg/mL onto HPLC sampler.
To my understanding, that volume is too large to analyze the purity.As a result of large volume injection, the main peak is trailed for about 3 min.There was a possibility of hiding some peaks in the long-trailed large peak. We loaded 10 uL of the sample at 2 mg/mL for purity analysis.
This is why EOS quality is so good, sole supplier could get 99%+. Korea CPHI C30. Welcome to visit.
GMP, ISO custom synthesis Medicinal Chemistry; FDA new API and Intermediates, HPLC 99%+, NMR, LCMS, MSDS, COA, MOA all we provided.
Teva, Novartis, Pfizer, Hikma, Glenmark, Gilead all Site Audit approved us.
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1.
Upadacitinib; ABT-494
CAS#: 1310726-60-3 (free base) , HPLC 99.5%, HNMR, MASS, MSDS, COA, MOA and DMF(CMC) document all we provided, More than 100g in stock.
CAS#: 1310726-60-3 (free base) , HPLC 99.5%, HNMR, MASS, MSDS, COA, MOA and DMF(CMC) document all we provided, More than 100g in stock.
Name: Upadacitinib
CAS#: 1310726-60-3 (free base)
Chemical Formula: C17H19F3N6O
Exact Mass: 380.1572
Molecular Weight: 380.3752
Elemental Analysis: C, 53.68; H, 5.04; F, 14.98; N, 22.09; O, 4.21
Synonym: ABT-494, Upadacitinib
ChemicalName:(3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide
InChi Key: WYQFJHHDOKWSHR-MNOVXSKESA-N
InChiCode:InChI=1S/C17H19F3N6O/c1-2-10-7-25(16(27)24-9-17(18,19)20)8-11(10)13-5-22-14-6-23-15-12(26(13)14)3-4-21-15/h3-6,10-11,21H,2,7-9H2,1H3,(H,24,27)/t10-,11+/m1/s1
SMILES Code: O=C(N1C[C@@H](CC)[C@@H](C2=CN=C3C=NC(NC=C4)=C4N32)C1)NCC(F)(F)F
Appearance: White to off-white solid powder
Appearance: White to off-white solid powder
Upadacitinib tartrate ; ABT-494
CAS#: 1607431-21-9 (tartarte) , HPLC 99.2%, HNMR, MASS, MSDS, COA, MOA and DMF(CMC) document all we provided, More than 100g in stock.
Name: Upadacitinib tartrate
CAS#: 1607431-21-9 (tartarte)
Chemical Formula: C21H25F3N6O7
Exact Mass:
Molecular Weight: 530.4612
Elemental Analysis: C, 47.55; H, 4.75; F, 10.74; N, 15.84; O, 21.11
Synonym: Upadacitinib tartrate, ABT-494, ABT 494, ABT494
ChemicalName: (3S,4R)-3-ethyl-4-(3H-imidazo(1,2-a)pyrrolo(2,3-e)pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide (2R,3R)-2,3-dihydroxybutanedioate
InChi Key: WQDBPGWQDBPVQZ-NBCXFSEXSA-N
InChi Code: InChI=1S/C17H19F3N6O.C4H6O6/c1-2-10-7-25(16(27)24-9-17(18,19)20)8-11(10)13-5-22-14-6-23-15-12(26(13)14)3-4-21-15;5-1(3(7)8)2(6)4(9)10/h3-6,10-11,21H,2,7-9H2,1H3,(H,24,27);1-2,5-6H,(H,7,8)(H,9,10)/t10-,11+;1-,2-/m11/s1
SMILES Code:O=C(N1C[C@@H](CC)[C@@H](C2=CN=C3C=NC(NC=C4)=C4N32)C1)NCC(F)(F)F.O=C(O)[C@H](O)[C@@H](O)C(O)=O
Appearance: White to off-white solid powder
Appearance: White to off-white solid powder
2.
Upadacitinib; ABT-494 Intermediates：
Upadacitinib, ABT494, Intermediate: 1428243-28-0, HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 1kg in stock.
Upadacitinib, ABT494, Intermediate:1428243-27-9, HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 1kg in stock.
Upadacitinib, ABT494, Intermediate: 1428243-26-8 , HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Upadacitinib, ABT494, Intermediate: tert-butyl 5-tosyl-5H-pyrrolo[2,3-b]pyrazin-2-ylcarbamate,
CAS: 1201187-44-1, HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than
10kg in stock.
Upadacitinib, ABT494, Intermediate: 2-Bromo-5-[(4-methylphenyl)sulfonyl]-5H-pyrrolo[2,3-b]pyrazine, CAS: 1201186-54-0, HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Upadacitinib, ABT494, Intermediate: 5-bromo-3-((trimethylsilyl)ethynyl)pyrazin-2-amine, CAS: 875781-41-2
, HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Upadacitinib, ABT494, Intermediate: 2-Amino-3,5-dibromopyrazine, CAS: 24241-18-7, HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Upadacitinib, ABT494, Intermediate: ethyl pent-2-ynoate, CAS: 55314-57-3
, HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Upadacitinib, ABT494, Intermediate:Carbamic acid,N-[5-[(4-methylphenyl)sulfonyl]-5H-pyrrolo[2,3-b]pyrazin-2-yl]-, ethyl este, CAS: 1869118-24-0
, HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Upadacitinib, ABT494, Intermediate: 2050038-81-6
, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 1kg in stock.
Upadacitinib, ABT494, Intermediate: 2095311-51-4
, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 1kg in stock.
Upadacitinib, ABT494, Intermediate: 2050038-84-9
, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 1kg in stock
Upadacitinib, ABT494, Intermediate:2,2,2-TrifluoroethylaMine, CAS: 753-90-2
, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 1kg in stock.
Upadacitinib, ABT494, Intermediate: (Z)-2-Pentenoic acid ethyl ester, CAS: 27805-84-1
, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 1kg in stock.
Upadacitinib, ABT494, Intermediate: (3R,4S)-1-[(benzyloxy)carbonyl]-4-ethylpyrrolidine-3-carboxylic acid, CAS: 1428243-25-7
, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
REFERENCES
1: Genovese MC, Smolen JS, Weinblatt ME, Burmester GR, Meerwein S, Camp HS, Wang L, Othman AA, Khan N, Pangan AL, Jungerwirth S. Efficacy and Safety of ABT-494, a Selective JAK-1 Inhibitor, in a Phase IIb Study in Patients With Rheumatoid Arthritis and an Inadequate Response to Methotrexate. Arthritis Rheumatol. 2016 Dec;68(12):2857-2866. doi: 10.1002/art.39808. PubMed PMID: 27390150; PubMed Central PMCID: PMC5132065.
2: Kremer JM, Emery P, Camp HS, Friedman A, Wang L, Othman AA, Khan N, Pangan AL, Jungerwirth S, Keystone EC. A Phase IIb Study of ABT-494, a Selective JAK-1 Inhibitor, in Patients With Rheumatoid Arthritis and an Inadequate Response to Anti-Tumor Necrosis Factor Therapy. Arthritis Rheumatol. 2016 Dec;68(12):2867-2877. doi: 10.1002/art.39801. PubMed PMID: 27389975; PubMed Central PMCID: PMC5132116.
3: Mohamed MF, Camp HS, Jiang P, Padley RJ, Asatryan A, Othman AA. Pharmacokinetics, Safety and Tolerability of ABT-494, a Novel Selective JAK 1 Inhibitor, in Healthy Volunteers and Subjects with Rheumatoid Arthritis. Clin Pharmacokinet. 2016 Dec;55(12):1547-1558. PubMed PMID: 27272171.
4: Semerano L, Decker P, Clavel G, Boissier MC. Developments with investigational Janus kinase inhibitors for rheumatoid arthritis. Expert Opin Investig Drugs. 2016 Dec;25(12):1355-1359. PubMed PMID: 27748152.
5: Nakayamada S, Kubo S, Iwata S, Tanaka Y. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419. Review. Erratum in: BioDrugs. 2016 Oct;30(5):483. PubMed PMID: 27577235.
6: Norman P. Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. doi: 10.1517/13543784.2014.918604. Review. PubMed PMID: 24818516.
EOS Med Chem, Medchem is Big
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2018. 4.18 Janpan CPHI, Attend
2018. 5.15 Israel Biomed, Attend
2018. 6. 20 China CPHI, W4E82
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2018. 10. 9 Spain World CPHI, Attend
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