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    • 9. 发明公开
    • New preparation of rosuvastatin, the useful intermediates thereof and preparation of the same
    • 罗维沙星的新制剂,其有用的中间体及其制备
    • KR20100131245A
    • 2010-12-15
    • KR20090050044
    • 2009-06-05
    • CHONG KUN DANG PHARM CORP
    • LEE HONG WOOPARK DAE JONGYOO CHOONG LEOLNAM DONG HYUKRYU HO HYUNGKIM DONG JIN
    • C07D239/42A61K31/505A61P3/06
    • C07D239/42C07C67/31C07C67/343C07C69/675C07C69/716C07D317/30C07D405/06C07D405/12C07D417/12
    • PURPOSE: A method for preparing a novel intermediate compound used for rosuvastatin is provided to obtain rosuvastatin hemicalcium salt. CONSTITUTION: A compound of chemical formula 3 is prepared by reacting a compound of chemical formula 2 with a compound of chemical formula 1 under the presence of base. The base is lithium(trimethylsilyl)amide, sodium bis(trimethylsilyl)amide or potassium(trimethylsilyl)amide. A method for preparing a compound of chemical formula 4 comprises: a step of removing dihydroxy group from 2-methyl-1-phenylpropane-2-yl 2-((4R,6S)-6-((E)-2-(4- (4-fluorophenyl)-6-isopropyl-2-(N-methyl methyl sulfonamido)pyrimidine-5-yl)vinyl)-2,2-dimethyl-1,3-dioxane-4-yl)acetate; a step of decomposing alpha,alpha-dimethylphenylethyl ester group of the product under the presence of base; a step of neutralizing under the presence of acid to obtain (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidine-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid; and a step of reacting the resultant with alkyl amine and pharmaceutically acceptable salt-producing reactant to obtain a compound of chemical formula 4.
    • 目的:提供一种制备用于瑞舒伐他汀的新型中间体化合物的方法,以获得瑞舒伐他汀半钙盐。 构成:化学式3的化合物通过化学式2的化合物与化学式1的化合物在碱的存在下反应来制备。 碱为锂(三甲基甲硅烷基)酰胺,双(三甲基甲硅烷基)氨基钠或(三甲基甲硅烷基)氨基钾。 制备化学式4的化合物的方法包括:从2-甲基-1-苯基丙烷-2-基2 - ((4R,6S)-6 - ((E)-2-(4 - (4-氟苯基)-6-异丙基-2-(N-甲基甲基亚磺酰氨基)嘧啶-5-基)乙烯基)-2,2-二甲基-1,3-二恶烷-4-基)乙酸乙酯; 在碱存在下分解产物中的α,α-二甲基苯乙基酯基的步骤; 得到(E)-7- [4-(4-氟苯基)-6-异丙基-2- [甲基(甲基磺酰基)氨基]嘧啶-5-基](3R,5S)的步骤在酸存在下中和, -3,5-二羟基庚-6-烯酸; 以及使所得物与烷基胺和药学上可接受的产生盐的反应物反应以获得化学式4的化合物的步骤。