1187594-09-7

  • Product Name:Baricitinib
  • Molecular Formula:C16H17N7O2S
  • Purity:99%
  • Molecular Weight:371.423
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Product Details:

CasNo: 1187594-09-7

Molecular Formula: C16H17N7O2S

Buy High Quality Top Purity Baricitinib 1187594-09-7 In Bulk Supply

  • Molecular Formula:C16H17N7O2S
  • Molecular Weight:371.423
  • PKA:11.66±0.50(Predicted) 
  • PSA:128.94000 
  • Density:1.6±0.1 g/cm3 
  • LogP:2.11438 

Baricitinib(Cas 1187594-09-7) Usage

Description

Baricitinib is an oral medication belonging to the class of Janus kinase (JAK) inhibitors. It acts by inhibiting the activity of JAK proteins, particularly JAK1 and JAK2, which play a crucial role in the signaling pathways of various interleukins, interferons, and growth factors involved in inflammatory processes.
Uses

Rheumatoid Arthritis: Baricitinib is indicated for the treatment of moderate to severe rheumatoid arthritis (RA) in adults who have responded poorly to at least one tumor necrosis factor (TNF) antagonist. It helps reduce inflammation and alleviate symptoms associated with RA, such as joint pain and swelling.

Alopecia Areata: Baricitinib has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of severe alopecia areata (AA) in adults. It helps promote hair regrowth by modulating the immune response involved in AA.

COVID-19: Baricitinib has been investigated for its potential use in the treatment of COVID-19. It has shown promise in reducing inflammation associated with severe COVID-19 and may also have antiviral effects by inhibiting SARS-CoV-2 endocytosis.

1187594-09-7 Relevant articles

Baricitinib for the treatment of rheumatoid arthritis

Satoshi Kubo,Shingo Nakayamada &Yoshiya Tanaka

Expert Review of Clinical Immunology Volume 12, 2016 - Issue 9

Five phase 3 trials of Baricitinib, a JAK1 and JAK2 inhibitor, have been performed and showed high clinical efficacy in patients with active RA and naïve to sDMARDs or an inadequate response to sDMARDs, MTX or bDMARDs.

Baricitinib: A Review in Rheumatoid Arthritis

Zaina T. Al-Salama & Lesley J. Scott

, Drugs, Volume 78, pages 761–772, (2018)

Baricitinib was generally well tolerated during up to 5.5 years’ treatment; the most commonly reported adverse drug reactions were upper respiratory tract infections, increased LDL cholesterol, nausea and thrombocytosis.

Baricitinib therapy in COVID-19: A pilot study on safety and clinical impact

Fabrizio Cantini Laura Niccoli Daniela Matarrese Emanuele Nicastri Paolo Stobbione Delia Goletti

, LETTERS TO THE EDITOR| VOLUME 81, ISSUE 2, P318-356, AUGUST 2020

The last consecutive patients with moderate COVID-19 pneumonia receiving standard of care therapy (lopinavir/ritonavir tablets 250 mg/bid and hydroxychloroquine 400 mg/day/orally for 2 weeks) admitted before the date of the first baricitinib-treated patient served as controls. Antibiotics were scheduled only in the case of suspected bacterial infection.

1187594-09-7 Process route

tert-butyl 4-{1-[3-(cyanomethyl)-1-(ethylsulfonyl)azetidin-3-yl]-1H-pyrazol-4-yl}-7H-pyrrolo[2.3-d]pyrimidine-7-carboxylate

tert-butyl 4-{1-[3-(cyanomethyl)-1-(ethylsulfonyl)azetidin-3-yl]-1H-pyrazol-4-yl}-7H-pyrrolo[2.3-d]pyrimidine-7-carboxylate

Baricitinib
1187594-09-7

Baricitinib

Conditions
Conditions Yield
With hydrogenchloride; In ethanol; at 40 - 45 ℃;
93%
With hydrogenchloride; In ethanol; at 40 - 45 ℃;
93%
In water; butan-1-ol; at 90 ℃;
92.7%
With trifluoroacetic acid; In dichloromethane; at 0 - 5 ℃; for 2h;
90.1%
2-(1-(ethanesulfonyl)-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)azetidine-3-yl)acetonitrile
1919837-50-5

2-(1-(ethanesulfonyl)-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)azetidine-3-yl)acetonitrile

4-chloro-1H-pyrrolo[2,3-d]pyrimidine
3680-69-1

4-chloro-1H-pyrrolo[2,3-d]pyrimidine

Baricitinib
1187594-09-7

Baricitinib

Conditions
Conditions Yield
With tetrakis(triphenylphosphine) palladium(0); potassium carbonate; In 1,4-dioxane; water; at 80 - 85 ℃; for 5h;
99%
With tetrakis(triphenylphosphine) palladium(0); cesium fluoride; In water; toluene; tert-butyl alcohol; at 100 ℃; for 48h; Concentration; Temperature; Solvent; Reagent/catalyst; Inert atmosphere;
90%
With potassium phosphate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH2Cl2; In tetrahydrofuran; water; at 90 ℃; for 19h; Autoclave; Inert atmosphere;
90%
With tetrakis(triphenylphosphine) palladium(0); cesium fluoride; In water; toluene; tert-butyl alcohol; for 48h; Reflux; Inert atmosphere;
84%

1187594-09-7 Upstream products

  • 1187594-13-3
    1187594-13-3

    2-[1-ethanesulfonyl-3-[4-(7-[(2-(trimethylsilyl)ethoxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl]acetonitrile

  • 1187595-90-9
    1187595-90-9

    (4-{1-[3-(cyanomethyl)-1-(ethylsulphonyl)azetidin-3-yl]-1H-pyrazol-4-yl}-7H-pyrrolo[2,3-d]pyrimidin-7-yl)methyl 2,2-dimethylpropanoate

  • 1153949-11-1
    1153949-11-1

    3-(cyanomethylene)azetidine-1-carboxylic acid tert-butyl ester

  • 1919837-50-5
    1919837-50-5

    2-(1-(ethanesulfonyl)-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)azetidine-3-yl)acetonitrile

1187594-09-7 Downstream products

  • 1187595-84-1
    1187595-84-1

    baricitinib phosphate

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