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    • 10. 发明公开
    • 엔테카비어 제조방법
    • ENTECAVIR的准备方法
    • KR1020120091971A
    • 2012-08-20
    • KR1020110023232
    • 2011-03-16
    • (주) 성운파마코피아주식회사 한서켐
    • 정인화장명식김기남
    • C07D473/18A61K31/522A61P31/20
    • Y02P20/55C07D473/18A61K31/522
    • PURPOSE: A method for preparing entecavir is provided to cheaply obtain the entecavir of high purity and high content. CONSTITUTION: A method for preparing entecavir comprises: a step of reacting a compound of chemical formula 2 with alpha-hydroxy acetyl halide to prepare a ketene cyclic compound of chemical formula 3; a step of ring opending and reducing the keten cyclic compound under the presence of a base catalyst to prepare a compound of chemical formula 4; a step of esterification, sharpless epoxidation, and ring opening of the compound of chemical formula 4 and introducing R2 as an alcohol protection group to prepare a compound of chemical formula 5; a step of alkylation of the compounds of chemical formulas 5 and 6 to prepare a compound of chemical formula 7; a step of introducing amine protection group R3 to the compound of chemical formula 7 to prepare a compound of chemical formula 8; a step of preparing alkene compound of chemical formula 10 through Witting or under the presence of acid catalyst; and a step of deprotecting the compound of chemical formula 10.
    • 目的:提供一种制备恩替卡韦的方法,以便廉价地获得高纯度和高含量的恩替卡韦。 构成:制备恩替卡韦的方法包括:使化学式2的化合物与α-羟基乙酰卤反应制备化学式3的烯酮环状化合物的步骤; 在碱催化剂存在下,使环化合物和环酮化合物还原,制备化学式4的化合物; 化学式4化合物的酯化,无水环氧化和开环步骤,引入R2作为醇保护基,制备化学式5的化合物; 化学式5和化合物6的烷基化步骤以制备化学式7的化合物; 向化学式7化合物引入胺保护基团R3以制备化学式8的化合物的步骤; 通过配制或在酸催化剂存在下制备化学式10的烯烃化合物的步骤; 和使化学式10的化合物脱保护的步骤。