School of Chemistry and Materials Science, Ludong University, Yantai, Shandong 264025, P. R. China.
College of Chemistry and Chemical Engineering, Yantai University, Yantai, Shandong 264005, P. R. China.
Org Lett. 2022 Jul 15;24(27):4886-4891. doi: 10.1021/acs.orglett.2c01680. Epub 2022 Jul 1.
The highly regioselective C-H hydroxylalkylation of purines and purine nucleosides within 10 min via the α-C(sp)-H functionalization of alcohols at room temperature is reported here for the first time. The reaction tolerated various functional groups, which have the potential for further modification to afford other valuable molecules. The reported method avoids metal catalysts, light, and protecting groups, giving a direct strategy to access 6-substitued alkylated purines and nucleosides with pharmaceutical bioactivities.
本文首次报道了在室温条件下通过醇的α-C(sp)-H 官能化，高区域选择性地在 10 分钟内实现嘌呤和嘌呤核苷的 C-H 羟烷基化。该反应可耐受各种功能基团，具有进一步修饰以获得其他有价值分子的潜力。所报道的方法避免了金属催化剂、光照和保护基团，为获得具有药物生物活性的 6-取代烷基化嘌呤和核苷提供了一种直接策略。
