四丁基氯化铵诱导的-异氰二芳基胺的级联自由基加成/环化反应：一种合成 11-三氟甲基二苯并二氮杂 的新方法。
Tetrabutylammonium Chloride-Induced Cascade Radical Addition/Cyclization of -Isocyanodiaryl Amines: A Novel Protocol for the Synthesis of 11-Trifluoromethylated Dibenzodiazepines.
机构信息
National Engineering Research Center for Carbohydrate Synthesis, Key Lab of Fluorine and Silicon for Energy Materials and Chemistry of Ministry of Education, Key Laboratory for Green Chemistry of Jiangxi Province, Jiangxi Normal University, Nanchang 330022 Jiangxi, China.
出版信息
J Org Chem. 2022 Dec 16;87(24):16542-16549. doi: 10.1021/acs.joc.2c02100. Epub 2022 Dec 1.
A straightforward protocol for the synthesis of 11-trifluoromethylated dibenzodiazepines has been developed via TBAC-induced trifluoromethylation/cyclization of -isocyanodiaryl amines using Togni's reagent as the trifluoromethyl source. This is the first report on the one-step construction of CF-containing dibenzodiazepine drug skeletons. Additionally, a series of 11-trifluoromethylated dibenzodiazepines were afforded in moderate to excellent yields under transition-metal-free conditions.
已经开发出一种通过 TBAC 诱导 -异氰二芳基胺的三氟甲基化/环化反应，使用 Togni 试剂作为三氟甲基源来合成 11-三氟甲基二苯并二氮杂的直链协议。这是关于一步构建含 CF 的二苯并二氮杂药物骨架的第一个报告。此外，在无过渡金属条件下，以中等至优异的收率得到一系列 11-三氟甲基二苯并二氮杂*。
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