利用苯炔实现苯环1,4-双官能化的研究
首发时间:2021-03-18
摘要:本论文以苯炔前体为原料,在简单苯炔发生亲核加成的基础上,将亲核反应与[5,5]-重排串联,一步实现了苯环的1,4-双官能化,突破了传统苯炔反应仅限于实现苯环邻位双官能团化的限制,为芳炔化学的发展开辟了新道路。并且,此结构为许多具有生物活性的分子或药物分子的基础结构,对后续苯炔化学在天然产物与药物分子的发展与应用提供了重要意义。
关键词: 芳炔 芳炔前体 [5,5]重排 1, 4-双官能化
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Study on 1,4-Difunctionalization of Benzene Ring Using Benzyne
Abstract:In this paper, based on the simple nucleophilic addition of benzyne, the nucleophilic reaction and [5,5] - rearrangement reaction were connected in series, and the 1,4-difunctionalization of benzene ring was realized in one step, which broke through the limitation of the traditional benzyne reaction only realizing the ortho bifunctionalization of benzene ring and opened up a new way for the development of aryne chemistry. Moreover, this structure is the basic structure of many bioactive molecules or drug molecules, and provides important significance for the subsequent development and application of phenylacetylene chemistry in natural products and drug molecules.
Keywords: Aryne aryne precursor [5,5] rearrangement 1,4-difunctionalization
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