摘要
泊沙康唑(posaconazole,1)化学名为4-[4-[4-[4-[[(3R,5R)-5-(2,4-二氟苯基)-5-(1,2,4-三唑-1-基甲基)氧杂戊环-3-基]甲氧基]苯基]哌嗪-1-基]苯基]-2-[(2S,3S)-2-羟基戊-3-基]-1,2,4-三唑-3-酮,结构中含有4个手性碳。CAS登记号为171228-49-2。泊沙康唑由Schering-Plough研发,2005年首次在德国上市,商品名为Noxafil。
■Posaconazole,(3R,5R)-4-[4-[4-[4-[5-(2,4-Difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)tetrahydrofuran-3-ylmethoxy]phenyl]piperazin-1-yl]phenyl]-2-[1(S)-ethyl-2(S)-hydroxypropyl]-3,4-dihydro-2H-1,2,4-triazol-3-one.CAS:171228-49-2.Posaconazole shows good antibacterial activities against a variety of bacteria,such as,cryptococcus neoformans,shenk spore silk,wool spore fungus,ball spore fungus,aspergillus species,sickle bacteria genera actinomycetes pedis and zygomycetes,etc.So it can be used for the prevention and treatment of invasive fungal infections and drug resistance or other drug ineffective invasive fungal infection.Posaconazole inhibits CYP51,a key enzyme of ergosterol,so it can interfere with the growth of fungal cells and play an anti-fungal role.This paper describes some common synthetic methods,and makes comments and synthetic diagrams.
出处
《中国药物化学杂志》
CAS
CSCD
北大核心
2020年第3期182-186,4,共6页
Chinese Journal of Medicinal Chemistry
