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CAS 1779-49-3
methyltriphenylphosphonium bromide
登记编号:EDOX-029、ROSU-033、VORI-022、ETON-003
应用背景(按来源药适应症)
肺栓塞甲苯磺酸艾多沙班静脉血栓栓塞甲苯磺酸艾多沙班中风甲苯磺酸艾多沙班栓塞甲苯磺酸艾多沙班静脉血栓形成甲苯磺酸艾多沙班缺血性卒中甲苯磺酸艾多沙班高血压瑞舒伐他汀钙/非马沙坦钾三水合物血脂障碍瑞舒伐他汀钙/非马沙坦钾三水合物高血压瑞舒伐他汀钙/替米沙坦高脂血症瑞舒伐他汀钙/替米沙坦纯合子家族性高胆固醇血症瑞舒伐他汀钙杂合子家族性高胆固醇血症瑞舒伐他汀钙高脂蛋白血症Ⅲ型瑞舒伐他汀钙动脉粥样硬化瑞舒伐他汀钙II型高脂蛋白血症瑞舒伐他汀钙高胆固醇血症瑞舒伐他汀钙真菌感染伏立康唑念珠菌血症伏立康唑念珠菌病伏立康唑曲霉菌属感染伏立康唑新型隐球菌感染伏立康唑镰刀菌感染伏立康唑避孕依托孕烯获得性免疫缺损综合征依托孕烯痛经依托孕烯血崩依托孕烯前列腺增生依托孕烯月经失调依托孕烯
来源药(使用该中间体的合成路线)
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 甲苯磺酸艾多沙班Edoxaban Tosilate Hydrate | Tier B · 提前布局 | 2028 |
| 瑞舒伐他汀钙/非马沙坦钾三水合物Fimasartan potassium trihydrate/Rosuvastatin calcium | Tier C · 观察 / 贸易 | - |
| 瑞舒伐他汀钙/替米沙坦Rosuvastatin Calcium/Telmisartan | Tier C · 观察 / 贸易 | - |
| 瑞舒伐他汀钙Rosuvastatin Calcium | Tier B · 提前布局 | - |
| 伏立康唑Voriconazole | Tier C · 观察 / 贸易 | - |
| 依托孕烯Etonogestrel | 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。
lithium 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylate→ethyl 3-bromo-2-oxopropanoate→cinnamamide→ethyl (E)-2-styryloxazole-4-carboxylate→(E)-2-styryloxazole-4-carbaldehyde→methyltriphenylphosphonium bromide→(E)-2-styryl-4-vinyloxazole→(E)-2-(2-styryloxazol-4-yl)ethan-1-ol→(E)-2-(2-(2-styryloxazol-4-yl)ethyl)isoindoline-1,3-dione→tert-butyl (E)-(2-(2-styryloxazol-4-yl)ethyl)carbamate→tert-butyl (E)-2-styryl-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-carboxylate→tert-butyl 2-formyl-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-carboxylate→5-(tert-butyl) 2-methyl 6,7-dihydrooxazolo[5,4-c]pyridine-2,5(4H)-dicarboxylate
N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide→sodium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate→ethyl (R)-4-cyano-3-hydroxybutanoate→ethyl (R)-3-((tert-butyldimethylsilyl)oxy)-4-cyanobutanoate→(R)-3-((tert-butyldimethylsilyl)oxy)-4-cyanobutanoic acid→tert-butyl (R)-3-((tert-butyldimethylsilyl)oxy)-4-cyanobutanoate→tert-butyl (R)-5-amino-3-((tert-butyldimethylsilyl)oxy)-5-oxopentanoate→(R)-5-(tert-butoxy)-3-((tert-butyldimethylsilyl)oxy)-5-oxopentanoic acid→methyl carbonochloridate→(S)-(R)-5-(tert-butoxy)-3-((tert-butyldimethylsilyl)oxy)-5-oxopentanoic (ethyl carbonic) anhydride→methyltriphenylphosphonium bromide→tert-butyl (R)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-6-(triphenyl-l5-phosphanylidene)hexanoate→tert-butyl (R,E)-3-((tert-butyldimethylsilyl)oxy)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-5-oxohept-6-enoate→tert-butyl (R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3-hydroxy-5-oxohept-6-enoate→tert-butyl (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate
N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide→methyl carbonochloridate→methyltriphenylphosphonium bromide→4-((tert-butyldimethylsilyl)oxy)dihydro-2H-pyran-2,6(3H)-dione→(R)-1-phenylethan-1-amine→(S)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-5-(((R)-1-phenylethyl)amino)pentanoic acid→(S)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-5-(((R)-1-phenylethyl)amino)pentanoic (methyl carbonic) anhydride→(R)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-N-((R)-1-phenylethyl)-6-(triphenyl-l5-phosphanylidene)hexanamide→(R,E)-3-((tert-butyldimethylsilyl)oxy)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-5-oxo-N-((R)-1-phenylethyl)hept-6-enamide→(R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3-hydroxy-5-oxo-N-((R)-1-phenylethyl)hept-6-enamide→(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxy-N-((R)-1-phenylethyl)hept-6-enamide
N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide→sodium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate→ethyl (R)-4-cyano-3-hydroxybutanoate→ethyl (R)-3-((tert-butyldimethylsilyl)oxy)-4-cyanobutanoate→(R)-3-((tert-butyldimethylsilyl)oxy)-4-cyanobutanoic acid→tert-butyl (R)-3-((tert-butyldimethylsilyl)oxy)-4-cyanobutanoate→tert-butyl (R)-5-amino-3-((tert-butyldimethylsilyl)oxy)-5-oxopentanoate→(R)-5-(tert-butoxy)-3-((tert-butyldimethylsilyl)oxy)-5-oxopentanoic acid→methyl carbonochloridate→(S)-(R)-5-(tert-butoxy)-3-((tert-butyldimethylsilyl)oxy)-5-oxopentanoic (ethyl carbonic) anhydride→methyltriphenylphosphonium bromide→tert-butyl (R)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-6-(triphenyl-l5-phosphanylidene)hexanoate→tert-butyl (R,E)-3-((tert-butyldimethylsilyl)oxy)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-5-oxohept-6-enoate→tert-butyl (R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3-hydroxy-5-oxohept-6-enoate→tert-butyl (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate
N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide→methyl carbonochloridate→methyltriphenylphosphonium bromide→4-((tert-butyldimethylsilyl)oxy)dihydro-2H-pyran-2,6(3H)-dione→(R)-1-phenylethan-1-amine→(S)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-5-(((R)-1-phenylethyl)amino)pentanoic acid→(S)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-5-(((R)-1-phenylethyl)amino)pentanoic (methyl carbonic) anhydride→(R)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-N-((R)-1-phenylethyl)-6-(triphenyl-l5-phosphanylidene)hexanamide→(R,E)-3-((tert-butyldimethylsilyl)oxy)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-5-oxo-N-((R)-1-phenylethyl)hept-6-enamide→(R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3-hydroxy-5-oxo-N-((R)-1-phenylethyl)hept-6-enamide→(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxy-N-((R)-1-phenylethyl)hept-6-enamide
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