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CAS 91424-38-3
(S)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-5-(((R)-1-phenylethyl)amino)pentanoic (methyl carbonic) anhydride
登记编号：ROSU-041
应用背景（按来源药适应症）
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
来源药（使用该中间体的合成路线）
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 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 | - |
合成路线中的位置（上下游链）
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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→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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