发明名称 PREPARATION METHOD OF FOSAMPRENAVIR DERIVATIVES AND RELEVANT INTERMEDIATE THEREOF
摘要 Preparation method of fosamprenavir derivatives is disclosed. The compound shown by formula II or its ammonium salt is reacted with a metal ion source in solvent to obtain the compound shown by formula Iii. After isolating and purifying, the compound shown by formula III is catalytically reduced to the compound shown by formula I. In the formula, X is metal ion. Preferably, the metal ion source is a calcium ion source, sodium ion source, or potassium ion source, and X is calcium ion, sodium ion, or potassium ion. The solvent is methanol, ethanol, n-propanol, isopropanol, n-butanol, or sec-butanol. The catalytic reduction is carried out by using hydrogen as a reducing agent in the presence of palladium on carbon catalyst. The ammonium salt is methylamine salt, dimethylamine salt, ethylamine salt, diethylamine salt, isopropylamine salt, dibutylamine salt, dipropylamine salt, t-butylamine salt, or dicyclohexylamine salt. The relevant intermediate of fosamprenavir derivatives in the preparation method is also provided. The preparation method of fosamprenavir derivatives reduces the cost, improves the productivity, and is applicable for large-scale popularization and application.
申请公布号 US2013225839(A1) 申请公布日期 2013.08.29
申请号 US201113881676 申请日期 2011.10.26
申请人 XU JIANKANG;YE MEIQI;CHEN BIN;XU QIAOQIAO;ZHEJIANG JIUHOU PHARMA SCIENCE & TECHNOLOGY CO., LTD. 发明人 XU JIANKANG;YE MEIQI;CHEN BIN;XU QIAOQIAO
分类号 C07F9/655 主分类号 C07F9/655
代理机构 代理人
主权项
地址