エルトロンボパグオラミン

化学名:エルトロンボパグオラミン

CAS番号.496775-62-3

英語名:Eltrombopag Olamine

CBNumberCB82495099

MFC27H29N5O5

MW503.56

MOL File496775-62-3.mol

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)

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

危険有害性情報のコード(GHS)

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).

エルトロンボパグオラミン生産企業

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

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エルトロンボパグ オラミン

危険有害性情報のコード(GHS)

エルトロンボパグ オラミン 化学特性,用途語,生産方法

エルトロンボパグ オラミン 生産企業

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

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特性,用途語,生産方法

エルトロンボパグオラミン生産企業

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