衍生化
磷杂茂
基质(水族馆)
化学
反应条件
组合化学
药物化学
立体化学
有机化学
催化作用
高效液相色谱法
地质学
海洋学
标识
DOI:10.1021/acs.joc.3c00567
摘要
An efficient method for the synthesis of 1-hydroxy-2,5-dihydrophosphole 1-oxides, a type of five-membered P-containing heterocyclic compound, is presented. The reaction was carried out through a [4C+1P] cyclization of 1,3-dienes with a combination of PBr3 and P(OMe)3 as the P(III) source. To compare with the reported methods, the protocol reported herein not only is much milder and more rapid but also displays a broad substrate scope and affords the products in high yields (50–94%). In addition, the reaction could be reliably scaled up at the gram-scale level and was demonstrated to be a versatile platform for flexible derivatization. Consequently, this method provides a general and reliable way for the synthesis of five-membered phosphole derivatives.
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