Roy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323, United States.
Org Lett. 2013 Apr 5;15(7):1536-9. doi: 10.1021/ol400320q. Epub 2013 Mar 14.
A robust and efficient protocol for the introduction of the dioxolanylethyl moiety onto various aryl and heteroaryl halides has been developed, providing cross-coupling yields up to 93%. Copper-catalyzed borylation of 2-(2-bromoethyl)-1,3-dioxolane with bis(pinacolato)diboron followed by treatment with potassium bifluoride provides the key organotrifluoroborate reagent.
已开发出一种将二氧戊环乙基部分引入各种芳基和杂芳基卤化物的稳健、高效的方法,提供高达 93%的交叉偶联产率。2-(2-溴乙基)-1,3-二氧戊环与频哪醇硼酸酯的铜催化硼酸化反应,随后用氟化钾处理,提供了关键的有机三氟硼酸盐试剂。