Vonoprazan fumarate
Vonoprazan fumarate 物理性質
- 貯蔵温度 :
- Store at -20°C
- 溶解性:
- insoluble in H2O; insoluble in EtOH; ≥18.9 mg/mL in DMSO
- 外見 :
- solid
- InChIKey:
- ROGSHYHKHPCCJW-WLHGVMLRSA-N
- SMILES:
- N1(S(C2=CC=CN=C2)(=O)=O)C(C2=CC=CC=C2F)=CC(CNC)=C1.C(O)(=O)/C=C/C(O)=O
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)
Vonoprazan fumarate 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 |
Vonoprazan fumarate 化学特性,用途語,生産方法
説明
Vonoprazan fumarate (Takecab®), discovered and developed by
Takeda and Otsuka, was approved by the PMDA of Japan in
December 2014, and is indicated for the treatment of gastric ulcer,
duodenal ulcer and reflux esophagitis. Vonoprazan fumarate has
a novel mechanism of action called potassium-competitive acid
blockers, which competitively inhibit the binding of potassium
ions to H+, K+-ATPase (also known as the proton pump) in the final
step of gastric acid secretion in gastric parietal cells. Vonoprazan
does not inhibit Na+, K+-ATPase activity even at concentrations 500
times higher than that of their IC50 values against gastric H+,
K+-ATPase activity. Furthermore, the drug is unaffected by the
gastric secretory state, unlike PPIs.
使用
Vonoprazan Fumarate is a novel potassium-?competitive acid blocker for the treatment of acid-?related diseases.
主な応用
Vonoprazan fumarate is an oral, newly synthesised potassium-competitive acid blocker (P-CAB) with antisecretory activity. It is also a proton pump inhibitor (PPI) reversibly inhibiting H+/K+, ATPase. It is mainly used in the treatment of acid-related diseases such as GERD and peptic ulcer disease.
合成
Commercially
available 2-fluoroacetophenone (283) was brominated to yield
a-bromo-acetophenone derivative 284. This compound was
treated with ethyl 2-cyanoacetate (285) under basic conditions
to provide ketoester 286 in essentially quantitative yield. Next,
intramolecular condensation of 286 upon treatment of 4 M HCl
furnished the tri-substituted pyrrole 287 in 53% yield. Reduction
of the chloride under hydrogenolytic conditions facilitated arrival
at pyrrole 288, albeit in just 18% yield. Subsequent diisobutylaluminium
hydride (DIBAL) reduction, followed by the oxidation with
tetrapropylammonium perruthenate (TPAP) and 4-methylmorpholine
N-oxide (NMMO) afforded the corresponding aldehyde 290 in 60% yield across the 2 steps. Next, N-pyrrole substitution with pyridine-
3-sulfonyl chloride 291 gave rise to N-sulfonylpyrrole 292 in
82% yield. Reductive amination of 292 afforded amine 293, which
was treated with fumaric acid (294) via co-crystallization to provide
vonoprazan fumarate (XXXVI) in 74% for the two steps.
Vonoprazan fumarate 上流と下流の製品情報
原材料
準備製品
Vonoprazan fumarate 生産企業
Global( 475)Suppliers
1260141-27-2()キーワード:
- 1260141-27-2
- 1-[5-(2-fluorophenyl)-1-pyridin-3-ylsulfonylpyrrol-3-yl]-N-methylmethanamine
- AK-438
- vonoprazan(tak-438)
- fuMarate vonoprazan
- 1H-Pyrrole-3-methanamine, 5-(2-fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-, 2-butenedioate (1:1)
- 5-(2-Fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-methanamine 2-butenedioate TAK 438
- vonaprazan(TK-438)
- TAK-438
Vonoprazan fumarate
- VONOPRAZAN FUMARATE (TAK-438);TAK-438
- TAK 438,Vonoprazan
- TAK-438
- 1-(5-(2-FLUOROPHENYL)-1-(PYRIDIN-4-YLSULFONYL)-1H-PYRROL-3-YL)-N-METHYLMETHANAMINE
- 4-Aminopyrazolo[3
- vomoprazan fumarate
- Vonoprazan Fumarate-D3Q: What is
Vonoprazan Fumarate-D3 Q: What is the CAS Number of
Vonoprazan Fumarate-D3
- Vonoprazan Vonoprazan onoprazan Vonoprazan fumarate
- Vonorasen fumarate
- Vonoprazan fumarate API
- Vonoprazan Fumarate
DISCONTINUED PLEASE SEE V767013
- TAK-438 ISO 9001：2015 REACH
- TAK-438 USP/EP/BP
- TAK-438,1260141-27-2 Fluorine Prazan
- 5-(2-Fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-methanamine 2-butenedioate (Vonoprazan fumarate)
- Wonarazan Fumarate
- CS-597
- TAK 438; TAK438
- Vonoprazan-025-Salt2
- Vonolazan Fumarate API
- Vonaprazan
- 5-(2-Fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-1H-pyrrole-3-methanamine 2-butenedioate (Vonoprazan)