모리니다졸

모리니다졸
모리니다졸 구조식 이미지
카스 번호:
92478-27-8
한글명:
모리니다졸
동의어(한글):
모리니다졸
상품명:
Morinidazole
동의어(영문):
Morinidazole;Morpholinenidazole impurity H;1-(2-methyl-5-nitro-1H-imidazol-1-yl)-3-morpholinopropan-2-ol;4-Morpholineethanol, α-[(2-methyl-5-nitro-1H-imidazol-1-yl)methyl]-;alpha-[(2-Methyl-5-nitro-1H-imidazol-1-yl)methyl]-4-morpholineethanol
CBNumber:
CB82716291
분자식:
C11H18N4O4
포뮬러 무게:
270.29
MOL 파일:
92478-27-8.mol

모리니다졸 속성

끓는 점
521.4±50.0 °C(Predicted)
밀도
1.44±0.1 g/cm3(Predicted)
저장 조건
Store at -20°C
용해도
DMSO : ≥ 100 mg/mL (369.97 mM)
산도 계수 (pKa)
14.14±0.20(Predicted)
물리적 상태
Solid
색상
White to off-white

안전

모리니다졸 C화학적 특성, 용도, 생산

개요

Morinidazole (迈灵达®), discovered and developed by Jiangsu Hansoh Pharmaceutical, was approved by the CFDA in February 2014. Morinidazole is a novel third generation 5-nitroimidazoleclass antimicrobial agent indicated for the treatment of amoebiasis and anaerobic bacterial infections including appendicitis and pelvic inflammatory disease. 5-Nitroimidazole antimicrobial drugs act via nitroreduction of the molecules in the pathogens; as an analog of metronidazole, morinidazole exhibits greater antiparasitic potency against Trichomonas vaginalis and amoebic protozoa, and relatively weaker toxicity in vitro and in preclinical studies compared with metronidazole.

Synthesis

The strategy to prepare morinidazole, which exists as a racemate, overlaps with that of ornidazole. Commercially available epichlorohydrin (176) was reacted with commercial 2-methyl-5-nitro-1H-imidazole (175) to provide ornidazole 177 in 51% yield. Next, epoxide 178 was obtained in 84% through the treatment of ornidazole 177 with TBAF in aqueous sodium hydroxide. Subsequently, the ring of epoxide 178 was opened with the treatment of morpholine (179) to afford morinidazole (XX) in 75% yield.

Synthesis_92478-27-8

모리니다졸 준비 용품 및 원자재

원자재

준비 용품


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