发明名称 METHOD OF PREPARING INTERMEDIATE OF SALMETEROL
摘要 A method of preparing an intermediate of salmeterol (Compound 1, 2-amino-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl) ethanol) includes: reacting compound 2 with 2-methoxypropene in a first organic solvent to produce a reaction solution including compound 3, compound 2 including a 2-bromo precursor of Compound 1; reacting compound 3 with a nitrogen source to produce compound 4; reacting compound 4 with sodium borohydride in a second organic solvent to produce compound 5; and debenzylating compound 5 by ammonium formate / palladium-carbon catalytic transfer hydrogenation in a third organic solvent to produce Compound 1. A method of preparing salmeterol includes preparing Compound 1, and reacting Compound 1 to prepare salmeterol.
申请公布号 WO2016054279(A1) 申请公布日期 2016.04.07
申请号 WO2015US53347 申请日期 2015.09.30
申请人 AMPHASTAR PHARMACEUTICALS, INC. 发明人 QIU, YINHUA;WU, ZHENGYUAN;CHEN, SONG;ZHANG, HAONING
分类号 C07C213/08;C07C213/10;C07C217/10;C07C217/28;C07C217/40 主分类号 C07C213/08
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