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Nintedanib Ethanesulfonate Salt

Product Name
Nintedanib Ethanesulfonate Salt
CAS No.
656247-18-6
Chemical Name
Nintedanib Ethanesulfonate Salt
Synonyms
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
Molecular Formula
C31H33N5O4.C2H6O3S
Formula Weight
649.75706
MOL File
656247-18-6.mol
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Nintedanib Ethanesulfonate Salt Property

form 
Yellow solid.
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Hazard and Precautionary Statements (GHS)

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Nintedanib Ethanesulfonate Salt Chemical Properties,Usage,Production

Description

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.

Definition

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

Nintedanib Ethanesulfonate Salt Preparation Products And Raw materials

Raw materials

Preparation Products

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Nintedanib Ethanesulfonate Salt Suppliers

Shanghai Jinyin Biological Technology Co., Ltd
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814527417@qq.com
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China
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Jinan XuanDe Chemical Co., Ltd.
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0531-88803958-
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0531-82777287
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xuandechem@126.com
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China
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192
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Chembest Research Laboratories Limited
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021-20908456-
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021-58180499
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sales@BioChemBest.com
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China
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5948
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Wuhu Sumu Pharmaceutical Technology Co., Ltd.
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-
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3145613242@qq.com
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China
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WuHu Linze pharmaceutical Co.,Ltd.
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-
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2030235803@qq.com
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China
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91
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58
Hubei Junxian Biotechnology Co., Ltd
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3464928989@qq.com
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China
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Nanjing Puxin Pharmaceutical Technology Co., Ltd
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Fax
QQ360829978
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puxinpharma_2017@126.com
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China
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239
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Anqing Benro pharmachem Technology Co.,Ltd.
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794263564@qq.com
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China
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Ningbo Risheng Pharmaceutical Technology Co., Ltd.
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0574-89132888
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2928184953@qq.com
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China
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47
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Shanghai Boyle Chemical Co., Ltd.
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86-21-57758967
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sales@boylechem.com
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China
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2926
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View Lastest Price from Nintedanib Ethanesulfonate Salt manufacturers

Hong Kong Tiansheng New Material Trading Co., Ltd
Product
Nintedanib Ethanesulfonate Salt 656247-18-6
Price
US $100.00/Kg/Bag
Min. Order
1KG
Purity
99%
Supply Ability
10kg
Release date
2021-09-15
Hong Kong Tiansheng New Material Trading Co., Ltd
Product
Nintedanib Ethanesulfonate Salt 656247-18-6
Price
US $100.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
100KG
Release date
2021-09-13
WUHAN FORTUNA CHEMICAL CO., LTD
Product
Nintedanib Ethanesulfonate Salt 656247-18-6
Price
US $0.00/g
Min. Order
1g
Purity
99%min HPLC
Supply Ability
1000G
Release date
2021-07-23

656247-18-6, Nintedanib Ethanesulfonate SaltRelated Search:


  • (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
  • 656247-18-6
  • 1217052-38-5
  • C31H33N5O4C2H6O3S
  • C33H39N5O7S
  • API