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J.Am.Chem.Soc.2017,139,12390~12393苯酚类化合物是一种重要的大宗化工品,是制备许多高分子材料、药物、天然产物以及染料的重要原料.然而,高化学选择性和高区域选择性制备地酚类衍生物却一直是合成化学领域中的挑战:第一,酚羟基具有较强的酸性和亲核性,使其反应位点多发生在酚羟基而非苯环上;第二,在亲电反应中,苯环中酚羟基的邻位和对位都具有很高的活性,从而降低了反应的区域选择性;第三,酚类是典型的富电子芳烃,在反应过程中容易氧化分解.中国科学院上海有机化学研究所王东辉课题组通过新颖的自由基反应设计,在铜的催化下,专一性地实现了自由酚类的邻位与
J.Am.Chem.Soc.2017,139,12390 ~ 12393 Phenol is an important bulk chemical and is an important raw material for preparing many macromolecular materials, drugs, natural products and dyes.However, high chemical selectivity And high selective preparation of phenolic derivatives has been a challenge in the field of synthetic chemistry: First, the phenolic hydroxyl group has a strong acid and nucleophilic, making its reaction sites occur in the phenolic hydroxyl rather than benzene ring ; Secondly, in the electrophilic reaction, the phenolic hydroxyl in the benzene ring has high activity in ortho-position and para-position, thus reducing the regioselectivity of the reaction; thirdly, the phenols are typical electron-rich aromatics. The reaction process is easy to oxidative decomposition. Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences Wang Donghui group through a novel free radical reaction design, under the catalysis of copper, specifically to achieve the free phenols ortho and