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4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇 |
CAS No.: |
147118-36-3 |
分子式: |
C16H20FN3O3S |
分子量: |
353.41 |
备注: |
中文名称4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇中文同义词4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇;4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇,罗素伐他汀钙中间体;N-[4-(4-氟苯基)-5-羟甲基-6-异丙基-2-嘧啶基]-N-甲基甲磺酰胺;5R-1-24-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇;4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰胺基)]-嘧啶-5-甲醇Z7;2-(N-甲基甲磺酰氨基)-4-(4-氟苯基)-5-(羟甲基)-6-异丙基嘧啶;英文名称:4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[(N-METHYL-N-METHYLSULFONYL)AMINO]PYRIMIDINE-5-YL-METHANOL;R-1-24-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇英文名称4-(4-Fluorophenyl)-6-isopropyl-2-[(N-methyl-n-methylsulfonyl)amino]pyrimidine-5-yl-methanol英文同义词4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-(N-METHYL-N-METHYLSULFONYLAMINO)PYRIMIDINE-5-METHANOL;4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[(N-METHYL-N-METHYLSULFONYL)AMINO]PYRIMIDINE-5-YL-METHANOL;4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-(N-METHYL-N-METHYLSULFONYLAMINO)PYRIMIDINE-5-ME;Z-7:4-(4-Fluorophenyl)-6-isopropyl-2-[(N-Methyl-n-Methylsulfonyl)aMino]pyriMidine-5-yl-Methanol;4-(4-Fluorophenyl)-6-isopropyl-2-[(N-Methyl-n-Methylsulfonyl)aMino]pyriMidine-5-yl-Methano;6-isopropyl-2-(N-Methyl-N-MethylsulphonylaMino)-;RosuvastatinCalciuMInterMediateZ74-(4-Fluorophenyl)-6-isopropyl-2-[(N-Methyl-n-Methylsulfonyl)aMino]pyriMidine-5-yl-Methanol;[4-(4-fluorophenyl0-6-isopropyl-2-(N-methyl-N-methylsulfonyl-amino)Chemicalbookpyrimidin-5-yl]methanoCAS号147118-36-3分子式C16H20FN3O3S分子量353.41EINECS号604-563-9相关类别瑞舒伐他汀钙及其中间体;瑞舒伐他汀钙中间体;杂质对照品;对照品-杂质对照品;瑞舒伐他汀;医药中间体;中间体;医药原料;瑞舒伐他汀中间体;化工中间体;Fluorineseries;INTERMEDIATESOFROSUVASTATIN;INTERMEDIATESOFROSUVASTATINCALCIUM;RosuvastatinCalciumanditsintermediates;Rosuvastatinintermediates;Heterocycles;Inhibitors;Intermediates;Intermediates&FineChemicals;Pharmaceuticals;Sulfur&SeleniumCompoundsMol文件147118-36-3.mol结构式4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇性质熔点137-140°C沸点538.3±60.0°C(Predicted)密度1.317±0.06g/cm3(Predicted)储存条件Sealedindry,RoomTemperature溶解度可溶于氯仿(少许)、甲醇(少许)形态固体酸度系数(pKa)13.02±0.10(Predicted)颜色白色至浅黄色至浅橙色CAS数据库147118-36-3(CASDataBaseReference)4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇用途与合成方法用途4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇是由日本盐野义公司研究开发的新一代他汀类降血脂药物,属于HMG-CoA还原酶抑制剂,可降低升高的低密度胆固醇、总胆固醇、甘油三酯和脱辅酶基蛋白B浓度,同时升高高密度胆固醇的浓度。可用于治疗原发性高胆固醇血症和混合型脂肪代谢障碍症及纯合家族性高胆固醇血症的综合治疗。与其他的他汀类降血脂药相比,瑞舒伐他汀具有疗效确切、使用方便安全、副作用小等优点,被称为“超级他汀”。制备向500mL三口烧瓶中加入270mL四氢呋喃、9.0g(240mmol)硼氢化钠和22.8g(60mmol)(HPLC:99.7%)嘧啶酯(II),降温至0℃,缓慢滴加34.2g(240mmol)三氟化硼乙醚络合物,升温至60℃保温反应20h,反应完毕,冷却至室温,往反应液缓慢加入盐酸(v/v=5%),搅拌1.5h后,加入饱和的NaHCO3调pH=7~8,CH2Cl2(60mL×2)萃取,分去水层,CH2Cl2层用无水硫酸钠搅拌干燥,过滤,滤液减压浓缩至干,得到浅黄色固体嘧啶醇(III),即4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇20.49g,收率96.7%。 |
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