3(2)-哒嗪酮的单氟甲基化和二氟甲基化
Mono- and Difluoromethylation of 3(2)-Pyridazinones.
作者信息
Zhu Ziyue, Tang Jiaqi, Kyriazakos Samantha, Knieb Alexander, Xu Yijie, Zhang Chao, Prakash G K Surya
机构信息
Loker Hydrocarbon Research Institute and Department of Chemistry, University of Southern California, Los Angeles, California 90089-1661, United States.
出版信息
Org Lett. 2024 Sep 12. doi: 10.1021/acs.orglett.4c03002.
A method for direct -monofluoromethylation of pyridazinones with -monofluoromethyl--phenyl-2,3,4,5-tetramethylphenylsulfonium triflate is disclosed. A method for the - and -difluoromethylated pyridazinones with TMSCFBr as the only promising difluorocarbene precursor is also reported. Substrates with various relevant functional groups, including analogues of Lynparza, are tolerated under both methods.
公开了一种用三氟甲磺酸单氟甲基-苯基-2,3,4,5-四甲基苯锍将哒嗪酮直接单氟甲基化的方法。还报道了一种以TMSCFBr作为唯一有前景的二氟卡宾前体将哒嗪酮进行单氟甲基化和二氟甲基化的方法。在这两种方法下，具有各种相关官能团的底物，包括Lynparza的类似物，都是耐受的。
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