エルトロンボパグ オラミン

エルトロンボパグ オラミン 化学構造式
496775-62-3
CAS番号.
496775-62-3
化学名:
エルトロンボパグ オラミン
别名:
エルトロンボパグ オラミン;エルトロンボパグ オラミン (JAN)
英語名:
Unii-4U07F515lg
英語别名:
Eltrombopag olamine;Eltrombopag Diolamine;EltroMbopag OlaMine API;Revolade;Sb 497115gr;Unii-4U07F515;ELTROMBOPAG OL;Unii-4U07F515lg;Eltrombopag API;Promacta Olamine
CBNumber:
CB82495099
化学式:
C27H29N5O5
分子量:
503.56
MOL File:
496775-62-3.mol

エルトロンボパグ オラミン 物理性質

貯蔵温度 :
under inert gas (nitrogen or Argon) at 2–8 °C
溶解性:
DMSO:56.33(Max Conc. mg/mL);99.76(Max Conc. mM)
DMF:1.0(Max Conc. mg/mL);1.77(Max Conc. mM)
DMF:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.44(Max Conc. mM)
Ethanol:0.1(Max Conc. mg/mL);0.18(Max Conc. mM)
外見 :
Powder
安定性::
Hygroscopic
InChIKey:
LQQUHOUXABUDJA-OUFJFOJPSA-N
SMILES:
C(N)CO.O=C1/C(/C(C)=NN1C1C=CC(C)=C(C)C=1)=N\NC1C=CC=C(C2C=CC=C(C(=O)O)C=2)C=1O
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
絵表示(GHS) GHS hazard pictograms
注意喚起語
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H412 長期的影響により水生生物に有害 水生環境有害性、慢性毒性 3 P273, P501
注意書き
P264 取扱い後は皮膚をよく洗うこと。
P264 取扱い後は手や顔をよく洗うこと。
P273 環境への放出を避けること。
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。
P305+P351+P338 眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。
P501 内容物/容器を...に廃棄すること。

エルトロンボパグ オラミン 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

エルトロンボパグ オラミン 化学特性,用途語,生産方法

効能

血小板減少症治療薬, トロンボポエチン受容体作動薬

商品名

レボレード (ノバルティスファーマ)

説明

Eltrombopag is used to treat low blood platelet counts in adults with chronic immune (idiopathic) thrombocytopenia (ITP), when certain other medicines, or surgery to remove the spleen, have not worked well enough.Eltrombopag has also been recently approved (late 2012) for the treatment of thrombocytopenia (low blood platelet counts) in patients with chronic hepatitis C to allow them to initiate and maintain interferon-based therapy.

使用

Treatment of chemotherapy-induced thrombocytopenia and treatment of immune thrombocytopenic purpura.

臨床応用

Eltrombopag olamine, a thrombopoietin receptor (TpoR) agonist, was approved in late 2008 for the once-daily, oral short-term and long-term treatment of adult patients with previously treated chronic idiopathic thrombocytopenic purpura (ITP). It is the first small-molecule TpoR agonist and was launched in the U.S. for this indication in 2009 by GlaxoSmithKline (GSK). Because eltrombopag is a small molecule, the drug is administered orally and has a reduced potential for causing an immune system reaction versus alternative protein-based therapies. In 2010, eltrombopag was approved in Europe for the long-term treatment of adult patients with previously treated chronic ITP.

合成

The synthesis began with the nitration of 2-bromophenol (39) with sodium nitrate and sulfuric acid in water at 10??C to give 2-bromo-6-nitrophenol (40) in 25% yield, which was methylated using methyl iodide and potassium carbonate in refluxing acetone providing 2-bromo- 6-nitroanisole (41) in 76% yield (the Scheme).40 Suzuki coupling of compound 41 with 3-carboxyphenyl boronic acid with Pd(PPh3)4 and 2 M sodium carbonate in refluxing dioxane gave 20-methoxy- 30-nitrobiphenyl-3-carboxylic acid (42) in 47% yield as a tan powder. Demethylation using 48% HBr (aq) in refluxing acetic acid resulted in a 79% yield of 20-hydroxy-30-nitrobiphenyl-3-carboxylic acid (43). The nitro group of compound 43 was reduced via catalytic hydrogenation at 50 psi at room temperature over Pd/C in mixed ethanol/3 M aq NaOH solution to give 30-amino-20-hydroxybiphenyl- 3-carboxylic acid (44) in quantitative yield. The intermediate 1-(3,4-dimethylphenyl)-3-methyl-2,5-dihydro-1Hpyrazol- 5-one (47) was prepared by condensing of 3,4-dimethylphenyl- hydrazine 45 with ethyl acetoacetate 46 with sodium acetate in refluxing acetic acid in 76% yield. Treatment of (44) with sodium nitrite in 1 M HCl at 5??C, followed by condensation with 1-(3,4-dimethylphenyl)-3-methyl-2,5-dihydro-1H-pyrazol-5-one (47) at a constant pH of 7¨C8 via the addition of sodium bicarbonate and ethanol afforded eltrombopag in 32% yield. Finally, eltrombopag was treated with hydroxyl ethylamine to give eltrombopag olamine (VIII).

説明図

エルトロンボパグ オラミン 上流と下流の製品情報

原材料

準備製品


エルトロンボパグ オラミン 生産企業

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エルトロンボパグ オラミン  スペクトルデータ(1HNMR)


496775-62-3(エルトロンボパグ オラミン)キーワード:


  • 496775-62-3
  • Sb 497115gr
  • Unii-4U07F515lg
  • 3'-[(2Z)-2-[1-(3,4-DiMethylphenyl)-1,5-dihydro-3-Methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid coMpd. with 2-aMinoethanol(1:2)
  • EltroMbopag diethanolaMine salt
  • EltroMbopag IMpurity
  • 2-aminoethanol with (Z)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylate (2:1)
  • Unii-4U07F515
  • 2-aminoethanol,3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid
  • 2-Aminoethanol (E)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydra
  • ELTROMBOPAG OLAMINE IH
  • 3'-[(2Z)-2-[1-(3,4-Dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid compd. with 2-aminoethanol
  • Revolade
  • ELTROMBOPAG OL
  • ELTROMBOPAG DIETHANOLAMINE SALT; PROMACTA; REVOLADE; SB-497115GR
  • 2-aminoethanol (Z)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylate
  • Eltrombopag Olamin
  • Eltrombopag ethanolamine
  • Promacta Olamine
  • 2-aminoethanolhemi((Z)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylate)
  • 2-aminoethanol,3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoicaci
  • Unii-4U07F515lg ISO 9001:2015 REACH
  • Eltrombopag Olamine (SB-497115GR)
  • ltrombopag Impurity 13
  • Eltrombopag OlamineQ: What is Eltrombopag Olamine Q: What is the CAS Number of Eltrombopag Olamine Q: What are the applications of Eltrombopag Olamine
  • Eltrombopag olamine
  • EltroMbopag OlaMine API
  • Eltrombopag Diolamine
  • 8-Benzothiazolecarboxaldehyde
  • 2-Aminoethan-1-ol hemi((Z)-3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylate)
  • 496775-62-3
  • エルトロンボパグ オラミン
  • エルトロンボパグ オラミン (JAN)
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