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ニンテダニブエタンスルホン酸塩

ニンテダニブエタンスルホン酸塩 化学構造式
656247-18-6
CAS番号.
656247-18-6
化学名:
ニンテダニブエタンスルホン酸塩
别名:
NINTEDANIB, ETHANESULFONATE SALT;ニンテダニブエタンスルホン酸塩;ニンテダニブエシラート;ニンテダニブエタンスルホン酸塩 (JAN)
英語化学名:
Nintedanib Ethanesulfonate Salt
英語别名:
Nintedani;BIBF-1120 esylate;BIBF 1120 esylate;Nintedanib esylate;Nintedanib (Ofev);BIBF 1120 BIBF-1120;Trinidad Neeb esylate;Intedanib ethanesulfonate;Nintedanib ethanesulfonate;Brand name OFEV. Vargatef.
CBNumber:
CB02509952
化学式:
C31H33N5O4.C2H6O3S
分子量:
649.75706
MOL File:
656247-18-6.mol

ニンテダニブエタンスルホン酸塩 物理性質

外見 :
Yellow solid.
CAS データベース:
656247-18-6

安全性情報

ニンテダニブエタンスルホン酸塩 価格 もっと(3)

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
富士フイルム和光純薬株式会社(wako) W01COBQJ-5714
(3Z)-2,3-Dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1h-indole-6-carboxylic acid methyl ester ethanesulfonate
656247-18-6 100mg ¥147600 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01FLC519772 Nintedanib, Ethanesulfonate Salt
Nintedanib Ethanesulfonate Salt
656247-18-6 1g ¥323400 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01FLC519772 Nintedanib, Ethanesulfonate Salt
Nintedanib Ethanesulfonate Salt
656247-18-6 2g ¥580800 2018-12-26 購入

ニンテダニブエタンスルホン酸塩 化学特性,用途語,生産方法

効能

抗線維化薬, チロシンキナーゼ阻害薬

商品名

オフェブ (日本ベーリンガーインゲルハイム)

説明

Nintedanib esylate is a potent, oral triple angiokinase inhibitor developed by Boehringer Ingelheim that targets proangiogenic and pro-fibrotic pathways mediated by the vascular endothelial growth factor receptor, fibroblast growth factor receptor and plateletderived growth factor receptor families, as well as Src and Flt-3 kinases. It was approved for the treatment of idiopathic pulmonary fibrosis (IPF), a condition in which the lungs become progressively scarred over time, by the US FDA in October 2014 and by the EMA in January 2015. The FDA granted nintedanib esylate fast-track, priority review, orphan product, and breakthrough designations. The drug was also approved by the EMA in November 2014 for treatment of non-small cell lung cancer in combination with docetaxel after first-line chemotherapy.

定義

ChEBI: An organosulfonate salt obtained by combining nintedanib with one molar equivalent of ethanesulfonic acid. A kinase inhibitor used for the treatment of idiopathic pulmonary fibrosis and cancer.

Chemical Synthesis

The synthesis of indolinone 197 commenced with commercial 4-chloro-3-nitro-benzoic acid (194)—esterification of which preceded displacement of the chloride by dimethyl malonate (195) in the presence of base to generate nitrobenzene 196. Hydrogenation of 196 under acidic conditions furnished 6-methyoxycarbonyl- substituted oxindole 197 by decarboxylative cyclization in 87% yield. Acylation of indolinone 197 with chloroacetic anhydride in refluxing toluene and subsequent condensation with trimethyl orthobenzoate resulted in indolone 198, which was isolated in 86% yield over the two-step sequence. While these two steps could reportedly be combined into a one-pot protocol using acetic anhydride as the solvent, the stepwise procedure was found to be more amenable for large-scale synthesis due to fewer complications with undesired side products. Subjection of 198 to methanolic potassium hydroxide followed by condensation with aniline fragment 199 in refluxing methanol and then exposure to aqueous ethanesulfonic acid in methanol provided nintedanib esylate (XXIII) in 82% over the three-step sequence.
Aniline fragment 199 was prepared in three steps and 82% overall yield via initial acylation of N-methyl-4-nitroaniline 200 with chloro acetylchloride followed by displacement of the a-amidochloride with N-methylpiperazine and hydrogenative reduction of the nitro group gave the desired aniline.183,184

ニンテダニブエタンスルホン酸塩 上流と下流の製品情報

原材料

準備製品


ニンテダニブエタンスルホン酸塩 生産企業

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656247-18-6(ニンテダニブエタンスルホン酸塩)キーワード:


  • 656247-18-6
  • (3Z)-2,3-Dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-indole-6-carboxylic acid methyl ester ethanesulfonate
  • Nintedanib ethanesulfonate
  • BIBF 1120 esylate
  • BIBF-1120 esylate
  • Nintedanib esylate
  • BIBF1120/nintedanib ethanesulfonate salt
  • Trinidad Neeb esylate
  • Intedanib ethanesulfonate
  • Nintedanib ethanesulfonate salt
  • Trinidad Neeb ethanesulfonate
  • Nintedanib(ethanesulfonic acid)
  • BIBF1120 ethanesulfonate salt
  • (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene
  • 1H-Indole-6-carboxylic acid,2,3-dihydro-3-[[[4-[methyl[(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]-phenylmethylene]-2-oxo-, methylester, (3Z)-, ethanesulfonate (1:1)
  • 1H-Indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester, (3Z)-, ethanesulfonate (1:1)
  • Nintedanib (Ofev)
  • (Z)-methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate
  • BIBF 1120 BIBF-1120
  • BIBF1120; BIBF 1120 BIBF-1120; NINTEDANIB ESYLATE. NINTEDANIB ETHANESULFONATE SALT; INTEDANIB; BRAND NAME OFEV. VARGATEF.
  • Brand name OFEV. Vargatef.
  • Nintedanib esylate. Nintedanib ethanesulfonate salt
  • Nintedanib Ethanesulfonate (Intedanib Ethanesulfonate)
  • Nintedani
  • NINTEDANIB, ETHANESULFONATE SALT
  • ニンテダニブエタンスルホン酸塩
  • ニンテダニブエシラート
  • ニンテダニブエタンスルホン酸塩 (JAN)
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