オルムチニブ
オルムチニブ 物理性質
- 比重(密度) :
- 1.336±0.06 g/cm3(Predicted)
- 貯蔵温度 :
- Store at -20°C
- 溶解性:
- insoluble in H2O; ≥9.11 mg/mL in EtOH with ultrasonic; ≥96.6 mg/mL in DMSO
- 外見 :
- crystalline solid
- 酸解離定数(Pka):
- 12.87±0.70(Predicted)
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)
オルムチニブ 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 |
オルムチニブ 化学特性,用途語,生産方法
効能
抗悪性腫瘍薬
説明
Olmutinib, codeveloped by
Boehringer Ingelheim and Hanmi Pharmaceutical Co., was
approved by the Korean Ministry of Food and Drug Safety
(MFDS) for treatment of locally advanced or metastatic EGFR
T790 M mutation-positive non-small cell lung cancer
(NSCLC). Olmutinib serves as a third-generation epidermal
growth factor receptor tyrosine kinase inhibitor (EGFR TKI),
which is being used as an oral therapy for patients who have
previously been treated with an alternate EGFR TKI. Firstand
second-generation EGFR TKIs, which bind reversibly and
irreversibly to the TK domain, respectively, are both generally
effective at onset of treatment but result in development of
resistance within the first year of treatment. Thirdgeneration
EGFR TKIs such as olmutinib have demonstrated
the ability to covalently bind to the kinase domain of EGFR
while sparing wild-type EGFR, leading to irreversible inhibition
of both EGFR mutations and the T790 M mutation, which is
linked to EGFR TKI resistance.
使用
Olmutinib is an epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) against non-small cell lung cancer (NSCLC).
合成
Synthetically, olmutinib can be accessed in two steps
beginning with 2,4-dichloro-thieno[3,2-d]pyrimidine (147), which is commercially available and can be
prepared in two steps from urea and 3-aminothiophene 2-
carboxylate. Nucleophilic addition of N-(3-hydroxyphenyl)-2-
propenamide (148) to 147 proceeded with complete
regioselectivity via treatment with K2CO3 in warm DMSO,
smoothly providing the desired diaryl ether 149 in 87% yield
after crystallization from isopropanol and water. From
149, substitution with commercially available piperazinyl aniline
150 under acidic heating conditions (DMA, IPA, TFA, 90 ??C)
provided olmutinib in 82% yield. After recrystallization,
olmutinib (XVI) was obtained in 60% overall yield and
99.1% purity.
オルムチニブ 上流と下流の製品情報
原材料
準備製品
オルムチニブ 生産企業
Global( 116)Suppliers
1353550-13-6(オルムチニブ)キーワード:
- 1353550-13-6
- HM71224
- HM-71224
- Olmutinib
- Olmutinib, HM71224
- N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide dihydrochloride monohydrate
- N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide
- N-[3-[[2-[[4-(4-Methyl-1-piperazinyl)phenyl]amino]thieno[3,2-d]pyrimidin-4-yl]oxy]phenyl]-2-propenamide
- HM71224, Olmutinib
- Olmutinib (HM61713, BI 1482694)
- poseltinib
- BI-1482694
- ZL-2303
- 1HM 71224
- EOS-62002
- N-(3-((2-((4-(4-METHYLPIPERAZIN-1-YL)PHENYL)AMINO)FURO[3,2-D]PYRIMIDIN-4-YL)OXY)PHENYL)ACRYLAMIDE
- CS-2203
- HM 61713;BI 1482694;HM61713;BI1482694
- Olmutinib (HM61713
- 2-Propenamide, N-[3-[[2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]thieno[3,2-d]pyrimidin-4-yl]oxy]phenyl]-
- Olmutinib free base
- OLMUTINIB (BI 1482694, HM71224)
- オルムチニブ
- N-{3-[(2-{[4-(4-メチルピペラジン-1-イル)フェニル]アミノ}チエノ[3,2-d]ピリミジン-4-イル)オキシ]フェニル}プロパ-2-エンアミド
- N-[3-[2-[4-(4-メチルピペラジン-1-イル)アニリノ]チエノ[3,2-d]ピリミジン-4-イル]オキシフェニル]プロペンアミド