兰州大学李云团队报道了()-Cyathin B2的对映选择性全合成——不对称双烯丙基硼化方法。相关研究成果于2024年8月28日发表在《美国化学会杂志》。

研究人员开发了一种强大的铂催化的，不对称二穿孔/不对称双烯丙基硼酸级联反应，用于在一次合成操作中以良好的收率和优异的对映体过量（ee）值，构建具有五个立体中心（包括三个季中心）的合成有用、高度官能化的醇酐。

利用这一关键串联方法的统一策略，从商业上可用的起始材料中，通过14个步骤实现了环亚烷二萜()-Cyathin B2的简洁不对称全合成，从而证明了其在合成含乙醇的天然产物和药物方面的巨大潜力。

附：英文原文

Title: Enantioselective Total Synthesis of ()-Cyathin B2: A Desymmetric Double-Allylboration Approach

Author: Jianping Wang, Jiacheng Yin, Hayatullah Imtiaz, Hongyu Wang, Yun Li

Issue&Volume: August 28, 2024

Abstract: A powerful Pt-catalyzed asymmetric diboration/desymmetric double-allylboration cascade reaction has been developed for the construction of synthetically useful, densely functionalized hydrindanes with five stereocenters, including three quaternary ones, in good yields and excellent enantiomeric excess (ee) values within a single synthetic operation. A unified strategy utilizing this key tandem methodology enabled the concise asymmetric total synthesis of cyathane diterpene ()-Cyathin B2 in 14 steps from commercially available starting materials, thereby demonstrating its remarkable potential in the synthesis of hydrindane-containing natural products and pharmaceuticals.

DOI: 10.1021/jacs.4c08042

Source: https://pubs.acs.org/doi/abs/10.1021/jacs.4c08042