Guo Ke, Zhang Shuaichen, Zhang Jing, Ren Yu, Chang Xiaoqiang, Sun Peng
State Key Laboratory for Quality Ensurance and Sustainable Use of Daodi Herbs, Institute of Chinese Materia Medica, Academy of Chinese Medical Sciences, Beijing 100700, China.
Artemisinin Research Center, Academy of Chinese Medical Sciences, Beijing 100700, China.
Molecules. 2025 Apr 16;30(8):1785. doi: 10.3390/molecules30081785.
Catalyst- and additive-free reactions for synthesizing valuable organic compounds have garnered significant attention in the context of sustainable development. As crucial structural motifs, allylic sulfones find extensive applications in pharmaceutical development and organic synthesis. Despite remarkable advances in allylic sulfone construction, catalyst-free and additive-free methodologies remain an underexplored frontier. Herein, we present an environmentally benign and atom-economical approach for synthesizing allylic sulfones by reacting electron-rich aryl-1,3-dienes with sulfinic acids, achieving yields of 10-94%. This transformation proceeds under ambient air at room temperature, eliminating the need for catalysts or additives. The protocol demonstrates exceptional regio- and chemo-selectivity, streamlined operational simplicity, and excellent scalability potential. This methodology establishes a sustainable and cost-effective paradigm for allylic sulfone synthesis, aligning with green chemistry principles.
在可持续发展的背景下，用于合成有价值有机化合物的无催化剂和无添加剂反应已引起广泛关注。烯丙基砜作为关键的结构基序，在药物开发和有机合成中有着广泛的应用。尽管烯丙基砜的构建取得了显著进展，但无催化剂和无添加剂的方法仍是一个未被充分探索的领域。在此，我们提出了一种环境友好且原子经济的方法，通过富电子芳基-1,3-二烯与亚磺酸反应来合成烯丙基砜，产率为10 - 94%。这种转化在室温环境空气中进行，无需催化剂或添加剂。该方案显示出优异的区域和化学选择性、简化的操作简便性以及出色的可扩展性潜力。这种方法为烯丙基砜的合成建立了一种可持续且具有成本效益的范例，符合绿色化学原则。
