College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, P. R. China.
Org Lett. 2020 Oct 2;22(19):7419-7423. doi: 10.1021/acs.orglett.0c02353. Epub 2020 Sep 18.
Here, we describe a highly selective Pd-catalyzed C(sp)-H biarylation of 2-methylbenzaldehydes using cyclic diaryliodonium salts as arylation reagents. The key strategy is the employment of -leucine as a bidentate transient directing group for the proximity-driven metalation to achieve reactivity and selectivity in C-H activation. Various functionalized biaryls bearing both aldehyde and iodine functional groups were prepared successfully, which could be further transformed into a wide range of compounds with potential applications in pharmaceutical chemistry and materials science.
在这里，我们描述了一种使用环状二芳基碘鎓盐作为芳基化试剂的高度选择性的 Pd 催化 2-甲基苯甲醛的 C(sp 2)-H 双芳基化反应。关键策略是使用 -亮氨酸作为双齿瞬态导向基团，通过临近驱动的金属化来实现 C-H 活化的反应性和选择性。成功制备了各种带有醛基和碘官能团的官能化联苯，它们可以进一步转化为具有潜在应用价值的药物化学和材料科学中的广泛化合物。
