올무티닙
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올무티닙 속성
- 밀도
- 1.336±0.06 g/cm3(Predicted)
- 저장 조건
- Store at -20°C
- 용해도
- insoluble in H2O; ≥9.11 mg/mL in EtOH with ultrasonic; ≥96.6 mg/mL in DMSO
- 물리적 상태
- 결정질 고체
- 산도 계수 (pKa)
- 12.87±0.70(Predicted)
- 색상
- Light yellow to yellow
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
올무티닙 C화학적 특성, 용도, 생산
개요
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.용도
Olmutinib is an epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) against non-small cell lung cancer (NSCLC).Synthesis
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.
올무티닙 준비 용품 및 원자재
원자재
2-Chlorothieno[3,2-d]pyriMidin-4(3H)-one
2,4-Dichlorothieno[3,2-d]pyrimidine
N-(3-히드록시페닐)아크릴아미드
2-메르캅토티에노[3,2-d]피리미딘-4(1H)온
2-(메틸술파닐)티에노[3,2-d]피리미딘-4(1H)온
4-(4-메틸피페라지노)아닐린
아크릴일클로라이드
준비 용품
올무티닙 공급 업체
글로벌( 117)공급 업체
| 공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
|---|---|---|---|---|---|
| Shandong Huisheng Import & Export Co., Ltd. | +86-13176845580 +86-13176845580 |
da@zhongda-biotech.com | China | 232 | 58 |
| Anhui Zhongda Biotechnology Co., Ltd | +8619956560829 |
justine@zhongda-biotech.com | China | 286 | 58 |
| Anhui Ruihan Technology Co., Ltd | +8617756083858 |
daisy@anhuiruihan.com | China | 973 | 58 |
| Nanjing Gold Pharmaceutical Technology Co. Ltd. | 025-84209270 15906146951 |
CHINA | 115 | 55 | |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32957 | 60 |
| BOC Sciences | +1-631-485-4226 |
inquiry@bocsci.com | United States | 19553 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 |
factory@coreychem.com | China | 29811 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 |
marketing@targetmol.com | United States | 32161 | 58 |
| Hubei Ipure Biology Co., Ltd | +8613367258412 |
ada@ipurechemical.com | China | 10319 | 58 |
| HONG KONG IPURE BIOLOGY CO.,LIMITED | 86 18062405514 18062405514 |
ada@ipurechemical.com | CHINA | 3461 | 58 |