OPC-67683
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OPC-67683 속성
- 녹는점
- 195-196℃
- 끓는 점
- 653.7±65.0 °C(Predicted)
- 밀도
- 1.45
- 저장 조건
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- 용해도
- 클로로포름(약간 용해됨), 에틸아세테이트(약간 용해됨, 초음파 처리)
- 산도 계수 (pKa)
- 3.99±0.20(Predicted)
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 색상
- 황백색에서 밝은 노란색까지
- 안정성
- 흡습성
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
OPC-67683 C화학적 특성, 용도, 생산
개요
Marketed by Otsuka, delamanid was approved in both the European Union and Japan in 2014 as part of combination therapies for multi-drug resistant tuberculosis (TB). Because delamanid exhibited no adverse drug–drug interactions, it has found utility as a combination therapy with standard antiretroviral drugs indicated for TB. Delamanid blocks mycolic acid biosynthesis in Mycobacterium tuberculosis, which allows its cell wall to be penetrated by small molecule antivirals.용도
Delamanid is a novel anti-tuberculosis medication that inhibits mycolic acid synthesis and shows potent in vitro and in vivo activity against drug-resistant strains of Mycobacterium tuberculosis.Synthesis
Piperidine 81 was concurrently prepared by first generating biaryl ether 79, which arose from a substitution reaction between pyridine N-oxide 77 and phenol 78 that proceeded in 86% yield. Next, removal of the N-oxide functionality by means of catalytic hydrogenation under mild pressure and neutral conditions afforded diaryl ether 80 in excellent yield. Reduction of the pyridine to the corresponding piperidine (81) was affected through the use of catalytic hydrogenation as well, this time under acidic conditions and elevated pressures relative to the N-oxide reduction. At this juncture, subjection of piperidine 81 to Buchwald¨C Hartwig conditions in the presence of diol subunit 82 delivered diol 83. A two-step elimination to deliver enantiopure epoxide 84 set the stage for an interesting cascade reaction to arrive at delamanid (XI) directly?a the initial alkylation of the epoxide by imidazole 85 proceeded under basic conditions with sodium acetate which then underwent an intramolecular nucleophilic substitution reaction by the liberated alcohol on the pendant imidazole chloride in the presence of sodium hydroxide. The reaction sequence proceeded in 73% yield to provide delamanid (XI) as a free base.
OPC-67683 준비 용품 및 원자재
원자재
준비 용품
OPC-67683 공급 업체
글로벌( 144)공급 업체
| 공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32480 | 60 |
| Biochempartner | 0086-13720134139 |
candy@biochempartner.com | CHINA | 967 | 58 |
| BOC Sciences | +1-631-485-4226 |
inquiry@bocsci.com | United States | 19553 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
sales@conier.com | China | 47465 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; |
factory@coreychem.com | China | 29826 | 58 |
| Shanxi Xuanran Import and Export Trade Co., Ltd. | +8617735180244 |
mike_yan@xuanranglobal.com | CHINA | 4022 | 58 |
| AFINE CHEMICALS LIMITED | 0571-85134551 |
info@afinechem.com | CHINA | 15377 | 58 |
| Dayang Chem (Hangzhou) Co.,Ltd. | 571-88938639 +8617705817739 |
info@dycnchem.com | CHINA | 52867 | 58 |
| Guangzhou TongYi biochemistry technology Co.,LTD | +8613073028829 |
mack@tongyon.com | China | 2996 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 |
sales@invivochem.cn | United States | 6393 | 58 |