重庆大学Hailong Yan研究小组实现了九元碳酸盐桥联的二芳基的阻转选择性构建。相关论文于2022年5月27日发表在《德国应用化学》杂志上。

该文中，团队通过利用联烯醌(VQM)中间体，开发了一种九元碳酸盐桥联的二芳基的阻转选择性构建方法。该方法可合成多种具有良好的药理特性产物，且收率高、对映体选择性好。

在随后的生物学测定中，几种药物通过线粒体相关的凋亡机制表现出较大的抗增殖活性。进一步的转变可产生更多的结构多样性，并可能激发开发功能分子的新思路。

附：英文原文

Title: Atroposelective Construction of Nine-Membered Carbonate Bridged Biaryls

Author: Shiqi Jia, Yuhong Tian, Xin Li, Pengfei Wang, Yu Lan, Hailong Yan

Issue&Volume: 2022-05-27

Abstract: We herein demonstrated an efficient method for the atroposelective construction of nine-membered carbonate bridged biaryls through vinylidene ortho-quinone methide (VQM) intermediates. Diverse products with desirable pharmacological features were synthesized in satisfying yields and good to excellent enantioselectivities. In subsequent bioassays, several agents showed considerable antiproliferative activity via the mitochondrial-related apoptosis mechanism. Further transformations produced more structural diversity and may inspire new ideas for developing functional molecules.

DOI: 10.1002/anie.202206501

Source: https://onlinelibrary.wiley.com/doi/10.1002/anie.202206501