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CAS 40018-26-6
1,4-dithiane-2,5-diol1,4-Dithiane-2,5-diol
登记编号：LAMI-016、EMTR-022、Ticlopidine-006
应用背景（按来源药适应症）
HIV感染多替拉韦/拉米夫定/艾酚福韦HIV感染拉米夫定/富马酸替诺福韦二吡呋酯慢性乙型肝炎拉米夫定/富马酸替诺福韦二吡呋酯HIV感染比克恩丙诺乙型肝炎比克恩丙诺HIV感染依非韦伦/拉米夫定/富马酸替诺福韦二吡呋酯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动脉闭塞性疾病盐酸噻氯匹定/银杏叶提取物脑血管疾病盐酸噻氯匹定/银杏叶提取物栓塞和血栓形成盐酸噻氯匹定/银杏叶提取物颈动脉狭窄盐酸噻氯匹定/银杏叶提取物
来源药（使用该中间体的合成路线）
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 多替拉韦/拉米夫定/艾酚福韦Dolutegravir/Lamivudine/Tenofovir Alafenamide | Tier C · 观察 / 贸易 | - |
| 拉米夫定/富马酸替诺福韦二吡呋酯Lamivudine/Tenofovir Disoproxil Fumarate | Tier C · 观察 / 贸易 | - |
| 比克恩丙诺Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate | Tier B · 提前布局 | - |
| 依非韦伦/拉米夫定/富马酸替诺福韦二吡呋酯Efavirenz/Lamivudine/Tenofovir Disoproxil Fumarate | Tier C · 观察 / 贸易 | - |
| 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 | - |
| 盐酸噻氯匹定/银杏叶提取物Ticlopidine Hydrochloride/Ginkgo Biloba Leaf Dried Extract | 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。
4-aminopyrimidin-2(1H)-one→(1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol→2-oxoacetic acid hydrate→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 2-oxoacetate→1,4-dithiane-2,5-diol→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-hydroxy-1,3-oxathiolane-2-carboxylate→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-acetoxy-1,3-oxathiolane-2-carboxylate→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-(4-amino-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate
4-aminopyrimidin-2(1H)-one→(1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol→2-oxoacetic acid hydrate→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 2-oxoacetate→1,4-dithiane-2,5-diol→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-hydroxy-1,3-oxathiolane-2-carboxylate→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-acetoxy-1,3-oxathiolane-2-carboxylate→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-(4-amino-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate
N-(5-fluoro-2-((trimethylsilyl)oxy)pyrimidin-4-yl)acetamide→1,4-dithiane-2,5-diol→2-oxoethyl benzoate→(5-acetoxy-1,3-oxathiolan-2-yl)methyl benzoate→(5-(4-acetamido-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl benzoate→4-amino-5-fluoro-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1H)-one→(5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl dihydrogen phosphate→((2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl dihydrogen phosphate
1,4-dithiane-2,5-diol→2-oxoacetic acid→5-hydroxy-1,3-oxathiolane-2-carboxylic acid→(2R,5R)-5-acetoxy-1,3-oxathiolane-2-carboxylic acid→(1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol→(2R,5R)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-acetoxy-1,3-oxathiolane-2-carboxylate→4-amino-5-fluoropyrimidin-2(1H)-one→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate
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
4-aminopyrimidin-2(1H)-one→(1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol→2-oxoacetic acid hydrate→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 2-oxoacetate→1,4-dithiane-2,5-diol→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-hydroxy-1,3-oxathiolane-2-carboxylate→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-acetoxy-1,3-oxathiolane-2-carboxylate→(2R,5S)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-(4-amino-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate
N-(5-fluoro-2-((trimethylsilyl)oxy)pyrimidin-4-yl)acetamide→1,4-dithiane-2,5-diol→2-oxoethyl benzoate→(5-acetoxy-1,3-oxathiolan-2-yl)methyl benzoate→(5-(4-acetamido-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl benzoate→4-amino-5-fluoro-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1H)-one→(5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl dihydrogen phosphate→((2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl dihydrogen phosphate
1,4-dithiane-2,5-diol→2-oxoacetic acid→5-hydroxy-1,3-oxathiolane-2-carboxylic acid→(2R,5R)-5-acetoxy-1,3-oxathiolane-2-carboxylic acid→(1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol→(2R,5R)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-acetoxy-1,3-oxathiolane-2-carboxylate→4-amino-5-fluoropyrimidin-2(1H)-one→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate
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
N-(5-fluoro-2-((trimethylsilyl)oxy)pyrimidin-4-yl)acetamide→1,4-dithiane-2,5-diol→2-oxoethyl benzoate→(5-acetoxy-1,3-oxathiolan-2-yl)methyl benzoate→(5-(4-acetamido-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl benzoate→4-amino-5-fluoro-1-(2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1H)-one→(5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl dihydrogen phosphate→((2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolan-2-yl)methyl dihydrogen phosphate
1,4-dithiane-2,5-diol→2-oxoacetic acid→5-hydroxy-1,3-oxathiolane-2-carboxylic acid→(2R,5R)-5-acetoxy-1,3-oxathiolane-2-carboxylic acid→(1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol→(2R,5R)-(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl 5-acetoxy-1,3-oxathiolane-2-carboxylate→4-amino-5-fluoropyrimidin-2(1H)-one→(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5S)-5-(4-amino-5-fluoro-2-oxopyrimidin-1(2H)-yl)-1,3-oxathiolane-2-carboxylate
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
3-Oxopentanedioic acid dimethyl diester→1,4-Dithiane-2,5-diol→Methyl 2-(2-methoxy-2-oxoethyl)thiophene-3-carboxylate→2-[3-(Hydroxymethyl)thiophen-2-yl]ethanol→2-(2-Hydroxyethyl)thiophene→2-(2-Bromoethyl)-3-(bromomethyl)thiophene→1-(2-Chlorophenyl)methanamine→5-(2-Chlorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine→2-(Carboxymethyl)thiophene-3-carboxylic acid→2-[2-(Methoxymethoxy)ethyl]thiophene→6,7-Dihydro-4H-thieno[3,2-c]pyran→2-[2-[(2-Methoxyethoxy)methoxy]ethyl]thiophene
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