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メシル酸レンバチニB

メシル酸レンバチニB 化学構造式
857890-39-2
CAS番号.
857890-39-2
化学名:
メシル酸レンバチニB
别名:
メシル酸レンバチニB;レンバチニブメシル酸塩;レンバチニブメシル酸塩 (JAN)
英語化学名:
lenvatinib Mesylate
英語别名:
CAT#A863437;E7080 Mesylate;envatinib MesyL;E7080;E-7080;E 7080;lenvatinib Mesylate;lenvatinib Mesylater;lenvatinib Methanesulfonate;lenvatinib Mesylate (E7080);Lenvatinib Mesylate fandachem;lenvatinib Mesylate USP/EP/BP
CBNumber:
CB42651170
化学式:
C22H23ClN4O7S
分子量:
522.95862
MOL File:
857890-39-2.mol

メシル酸レンバチニB 物理性質

安全性情報

メシル酸レンバチニB 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) W01COBQV-5519 メシル酸レンバチニb
Lenvatinib mesylate
857890-39-2 250mg ¥39600 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01COBQV-5519 メシル酸レンバチニb
Lenvatinib mesylate
857890-39-2 1g ¥97200 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01COBQV-5519 メシル酸レンバチニb
Lenvatinib mesylate
857890-39-2 5g ¥291600 2018-12-26 購入

メシル酸レンバチニB 化学特性,用途語,生産方法

効能

抗悪性腫瘍薬, 受容体チロシンキナーゼ阻害薬

商品名

レンビマ (エーザイ)

説明

Developed by Eisai Inc., lenvatinib mesylate is a vascular endothelial growth factor receptor (VEGF) inhibitor which has activity against VEGF subtypes 1, 2, and 3 and was approved by the FDA in 2015 for the treatment of differentiated thyroid cancer that is either locally recurrent, metastatic, or progressive and did not respond to radioactive iodine treatment. In May 2016, the FDA approved the drug as a combination therapy with everolimus for the treatment of advanced renal cell carcinoma. Because VEGF (and fibroblast growth factor receptors, known as FGFRs) are thought to play a role in cardiovascular signaling pathways, VEGF2R and FGFR inhibition are thought to be the mechanisms behind the primary side effect of lenvatinib mesylate, which is hypertension.

使用

E7080 (Lenvatinib) is a multi-target inhibitor of VEGFR2 and VEGFR3 with IC50 of 4 nM and 5.2 nM, respectively.

定義

ChEBI: A methanesulfonate salt obtained by reaction of lenvatinib with one molar equivalent of methanesulfonic acid. A multi-kinase inhibitor and orphan drug used (as its mesylate salt) for the treatment of various types of thyroid cancer that do not respond to r dioiodine.

Chemical Synthesis

Starting from commercial aniline 193, a substitution reaction under neutral conditions in warm isopropyl alcohol with a commercial vinyl methoxy derivative of Meldrum’s acid (194) produced enamine 195 in good yield. Next, subjection of 195 to DOWTHERM A at 190 °C affected an intramolecular cyclizative substitution reaction, followed by loss of acetone, and a decarboxylation reaction to furnish quinolone 196. This cyclization reaction, which is a variant of the Conrad-Limpach reaction, is particularly noteworthy given the temperature and pH at which it takes place. Conrad- Limpach cyclizations typically proceed under basic conditions at temperatures well above 240 °C. However, a process was developed by Zeneca in 2004 which involved subjecting 195 to the DOWTHERM heat transfer fluid (commercially available from Dow and Sigma-Aldrich, consisting of a eutectic mixture of biphenyl and diphenyl oxide) allowed the team to lower the temperature required for the reaction, clearly observe bubbling of gas indicating the progress of the reaction, and simple cooling and treatment with ether to facilitated precipitate formation. The resulting solid could be collected by filtration and required no additional purification on scale in 80% yield. Quinoline 196 was then converted to the corresponding chloride using thionyl chloride in refluxing DMF, and the resulting ester 197 was converted to the corresponding amide through the use of 28% aqueous ammonia in warm ethanol, which ultimately produced the key chloroquinoline lenvatinib subunit 198 in 80% yield from 197.
       
Commercial aminophenol 199 was converted to the corresponding carbamate through the use of phenyl chloroformate in essentially quantitative yield prior to subjection to cyclopropylamine in chilled DMF, which ultimately furnished urea 201 in 77% overall yield from 200. Next, exposure of phenol 201 to chloroquinoline 198 in the presence of potassium t-butoxide followed by treatment with methanesulfonic acid and acetic acid resulted in clean formation of lenvatinib mesylate (XXV) in 96% yield across the two-step sequence.
QQ截图20210205151737.jpg

メシル酸レンバチニB 上流と下流の製品情報

原材料

準備製品


メシル酸レンバチニB 生産企業

Global( 220)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Jinan Ande Pharmaceutical Co.,Ltd.
+8613256107535
andepharm@163.com CHINA 208 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58
Henan DaKen Chemical CO.,LTD.
+86-371-66670886
info@dakenchem.com China 20918 58
Jinan Xinke Pharmaceutical Sci.&Tech. Co.,Ltd.
+8618660188356 +86-531-88259693
maguanglei@xinkeyiyao.com;Tracy.li@xinkeyiyao.com CHINA 29 58
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8909 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26751 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 341 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29954 58

857890-39-2(メシル酸レンバチニB)キーワード:


  • 857890-39-2
  • lenvatinib Methanesulfonate
  • E7080 Mesylate
  • 4-[3-Chloro-4-[[(cyclopropylamino)carbonyl]amino]phenoxy]-7-methoxy-6-quinolinecarboxamide monomethanesulfonate
  • 4-[3chloro-4-(N'-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate
  • CAT#A863437
  • Lenvatinib Mesylate,Amadis Chemical offer CAS#857890-39-2
  • lenvatinib Mesylate
  • E7080;E-7080;E 7080
  • maltitol E:candyli(at)speedgainpharma(dot)com
  • LENVATINIB MESYLATE (E7080 MESYLATE)
  • 4-[3-chloro-4-(N'-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide mesylate
  • lenvatinib Mesylate (E7080)
  • 6-Quinolinecarboxamide,4-[3-chloro-4-[[(cyclopropylamino)carbonyl]amino]phenoxy]-7-methoxy-,monomethanesulfonate
  • envatinib MesyL
  • Lenvatinib Mesylate fandachem
  • lenvatinib Mesylate USP/EP/BP
  • lenvatinib Mesylater
  • メシル酸レンバチニB
  • レンバチニブメシル酸塩
  • レンバチニブメシル酸塩 (JAN)
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