萘醌催化胺类有氧氧化合成稠合嘧啶-4(3)-酮：一种合成布查拉丁和西地那非的汇聚式合成路线。
-Naphthoquinone-catalyzed aerobic oxidation of amines to fused pyrimidin-4(3)-ones: a convergent synthetic route to bouchardatine and sildenafil.
作者信息
Kim Kyeongha, Kim Hun Young, Oh Kyungsoo
机构信息
Center for Metareceptome Research, Graduate School of Pharmaceutical Sciences, Chung-Ang University 84 Heukseok-ro, Dongjak Seoul 06974 Republic of Korea
出版信息
RSC Adv. 2020 Aug 21;10(52):31101-31105. doi: 10.1039/d0ra06820a.
Abstract
A facile access to fused pyrimidin-4(3)-one derivatives has been established by using the metal-free -naphthoquinone-catalyzed aerobic cross-coupling reactions of amines. The utilization of two readily available amines allowed a direct coupling strategy to quinazolinone natural product, bouchardatine, as well as sildenafil (Viagra™) in a highly convergent manner.
摘要
通过使用无金属的萘醌催化的胺的需氧交叉偶联反应，已建立了一种简便合成稠合嘧啶-4(3)-酮衍生物的方法。利用两种易于获得的胺，能够以高度汇聚的方式直接将喹唑啉酮天然产物布查拉丁以及西地那非（伟哥™）进行偶联。
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