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CAS 764659-73-6
(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate oxalate
登记编号：EMTR-039
应用背景（按来源药适应症）
HIV感染比克恩丙诺乙型肝炎比克恩丙诺HIV感染恩曲他滨/富马酸磷丙替诺福韦获得性免疫缺损综合征恩曲他滨/富马酸磷丙替诺福韦进行性多病灶脑白质病恩曲他滨/富马酸磷丙替诺福韦HIV感染恩曲他滨/盐酸利匹韦林/富马酸替诺福韦二吡呋酯
来源药（使用该中间体的合成路线）
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 比克恩丙诺Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate | Tier B · 提前布局 | - |
| 恩曲他滨/富马酸磷丙替诺福韦Emtricitabine/Tenofovir Alafenamide Fumarate | Tier B · 提前布局 | - |
| 恩曲他滨/盐酸利匹韦林/富马酸替诺福韦二吡呋酯Emtricitabine/Rilpivirine Hydrochloride/Tenofovir Disoproxil Fumarate | Tier B · 提前布局 | - |
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。
5-fluoro-N-(trimethylsilyl)-2-((trimethylsilyl)oxy)pyrimidin-4-amine→1,4-dithiane-2,5-diol→2-oxoacetic acid→(1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 2-oxoacetate→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-hydroxy-1,3-oxathiolane-2-carboxylate→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5R)-5-chloro-1,3-oxathiolane-2-carboxylate→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate oxalate→4-amino-5-fluoro-1-((2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1H)-one hydrochloride
5-fluoro-N-(trimethylsilyl)-2-((trimethylsilyl)oxy)pyrimidin-4-amine→1,4-dithiane-2,5-diol→2-oxoacetic acid→(1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 2-oxoacetate→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-hydroxy-1,3-oxathiolane-2-carboxylate→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5R)-5-chloro-1,3-oxathiolane-2-carboxylate→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate oxalate→4-amino-5-fluoro-1-((2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1H)-one hydrochloride
5-fluoro-N-(trimethylsilyl)-2-((trimethylsilyl)oxy)pyrimidin-4-amine→1,4-dithiane-2,5-diol→2-oxoacetic acid→(1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 2-oxoacetate→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-hydroxy-1,3-oxathiolane-2-carboxylate→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5R)-5-chloro-1,3-oxathiolane-2-carboxylate→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate oxalate→4-amino-5-fluoro-1-((2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1H)-one hydrochloride
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