4-nitrophenyl phosphorodichloridate（CAS 777-52-6）中间体

应用背景（按来源药适应症）

丙型肝炎索磷布韦/维帕他韦慢性丙型肝炎索磷布韦/维帕他韦终末期肾脏病索磷布韦/维帕他韦肝脏移植排斥索磷布韦/维帕他韦肾脏移植排斥索磷布韦/维帕他韦心脏衰竭索磷布韦/维帕他韦慢性丙型肝炎索磷布韦丙型肝炎索磷布韦慢性乙型肝炎索磷布韦戊型肝炎病毒感染索磷布韦肝硬化索磷布韦门静脉高血压索磷布韦肝癌普瑞拉滨肝细胞癌普瑞拉滨线粒体疾病普瑞拉滨胆管上皮癌普瑞拉滨

来源药（使用该中间体的合成路线）

品种	梯队	到期年
索磷布韦/维帕他韦Sofosbuvir/Velpatasvir	Tier B · 提前布局	-
索磷布韦Sofosbuvir	Tier B · 提前布局	-
普瑞拉滨Pracytarabine	Tier C · 观察 / 贸易	-

合成路线中的位置（上下游链）

按路线登记顺序排列，左→右为合成方向；高亮为当前 CAS，其余可点击跳转对应档案。

索磷布韦/维帕他韦原研路线步数：6总收率：57 mg

1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyltetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione→(S)-isopropyl 2-aminopropanoate hydrochloride→1-((2R,3R,4R,5R)-5-(((tert-butyldimethylsilyl)oxy)methyl)-3-fluoro-4-hydroxy-3-methyltetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione→4-oxopentanoic anhydride→(2R,3R,4R,5R)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-4-methyltetrahydrofuran-3-yl 4-oxopentanoate→(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-2-(hydroxymethyl)-4-methyltetrahydrofuran-3-yl 4-oxopentanoate→(S)-isopropyl 2-(((R)-(4-nitrophenoxy)(phenoxy)phosphoryl)amino)propanoate→(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-2-((((S)-(((S)-1-isopropoxy-1-oxopropan-2-yl)amino)(phenoxy)phosphoryl)oxy)methyl)-4-methyltetrahydrofuran-3-yl 4-oxopentanoate→phenol→4-nitrophenyl phosphorodichloridate

索磷布韦原研路线步数：6总收率：57 mg

1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyltetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione→(S)-isopropyl 2-aminopropanoate hydrochloride→1-((2R,3R,4R,5R)-5-(((tert-butyldimethylsilyl)oxy)methyl)-3-fluoro-4-hydroxy-3-methyltetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione→4-oxopentanoic anhydride→(2R,3R,4R,5R)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-4-methyltetrahydrofuran-3-yl 4-oxopentanoate→(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-2-(hydroxymethyl)-4-methyltetrahydrofuran-3-yl 4-oxopentanoate→(S)-isopropyl 2-(((R)-(4-nitrophenoxy)(phenoxy)phosphoryl)amino)propanoate→(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-2-((((S)-(((S)-1-isopropoxy-1-oxopropan-2-yl)amino)(phenoxy)phosphoryl)oxy)methyl)-4-methyltetrahydrofuran-3-yl 4-oxopentanoate→phenol→4-nitrophenyl phosphorodichloridate

普瑞拉滨原研路线步数：5总收率：2.55 g

(E)-N'-(1-((2R,3S,4R,5R)-3,4-bis((tert-butyldimethylsilyl)oxy)-5-((((2R,4S)-2-oxido-4-(pyridin-4-yl)-1,3,2-dioxaphosphinan-2-yl)oxy)methyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)-N,N-dimethylformimidamide→ethyl 3-hydroxy-3-(pyridin-4-yl)propanoate→N,N-dimethyl-L-phenylalanine→(S)-3-ethoxy-3-oxo-1-(pyridin-4-yl)propyl dimethyl-L-phenylalaninate→(S)-1-(pyridin-4-yl)propane-1,3-diol→4-nitrophenyl phosphorodichloridate→(2S,4S)-2-(4-nitrophenoxy)-4-(pyridin-4-yl)-1,3,2-dioxaphosphinane 2-oxide→(E)-N'-(1-((2R,3S,4R,5R)-3,4-bis((tert-butyldimethylsilyl)oxy)-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)-N,N-dimethylformimidamide

本站可供应的对应中间体

同 CAS 多家在售供应横向对比；价格区间为供应方挂牌口径，实价以询价确认为准。

供应商	产品	价格区间	最小起订	货期	资质	操作
Unibest Taizhou GMP-like Site	2'-Deoxy-2'-fluoro-2'- Methyl-N-(phenylcarbonyl) cytidine Pharmaceutical Intermediates	询价	询价	询价	—
Qualified Partner — East China API Works	2'-deoxy-2'-fluoro-2'-C-methyluridine Pharmaceutical Intermediates	询价	询价	询价	—