Selective Phosphoramidation and Phosphonation of Benzoxazoles via Sequence Control
Selective Phosphoramidation and Phosphonation of Benzoxazoles via Sequence Control
复制标题
通过序列控制对苯并恶唑进行选择性磷酰胺化和磷膦化
DOI：
10.1021/acs.orglett.7b00726
复制
发表时间：
2017-05-05
期刊：
影响因子：
5.2
通讯作者：
Cai, Hu
中科院分区：
文献类型：
--
作者：
Huang, Ling;Gong, Jiuhan;Cai, Hu
研究了亚磷酸三烷基酯在碘存在下苯并恶唑的选择性磷酰胺化和膦酸化反应。在反应中，在室温下，10分钟内完成的转化和底物的耐受性很好，2-取代唑可以提供季碳中心的产品。重要的是，亚磷酸酯可以选择性地引入到苯并恶唑的C-和N-位，通过控制添加顺序和底物的比例。
A selective phosphoramidation and phosphonation of benzoxazole was developed with trialkyl phosphites in the presence of iodine under mild conditions. In the reaction, the transformation completes in 10 min at room temperature and the substrates are well tolerant, as 2-substituted azoles could afford the quaternary carbon-centered products. Significantly, phosphites could be selectively introduced into the C- and N-positions of the benzoxazoles by controlling the addition sequence and the ratio of substrates.