通过 -杂环卡宾催化的自由基接力实现乙烯基芳烃的有机催化三组分酰基二氟甲基化反应。
Organocatalytic Three-Component Acyldifluoromethylation of Vinylarenes via -Heterocyclic Carbene-Catalyzed Radical Relay.
机构信息
School of Chemistry and Pharmaceutical Sciences, State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, Guangxi Normal University, Guilin, Guangxi 541004, P. R. China.
Department of Chemistry, The Chinese University of Hong Kong, New Territories, Hong Kong, P. R. China.
出版信息
Org Lett. 2022 Jul 8;24(26):4840-4844. doi: 10.1021/acs.orglett.2c02093. Epub 2022 Jun 27.
We herein describe an -hetercyclic carbene-catalyzed three-component acyldifluoromethylation of vinylarenes, aldehydes, and NaSOCFH. This organocatalytic approach provides a practical route for the synthesis of pharmaceutically relevant α-aryl-β-difluormethyl ketones without the need for transition metals or photocatalysts. The late-stage acyldifluoromethylation of drug analogues was also demonstrated. The reaction design employs NaSOCFH as the source of the CFH radical in the presence of an oxidant for the radical relay.
我们在此描述了一种 -杂环卡宾催化的乙烯基芳烃、醛和 NaSOCFH 的三组分酰基二氟甲基化反应。这种有机催化方法为合成具有药物相关性的 α-芳基-β-二氟甲基酮提供了一种实用的途径，无需使用过渡金属或光催化剂。还展示了药物类似物的后期酰基二氟甲基化反应。该反应设计在氧化剂存在下使用 NaSOCFH 作为 CFH 自由基的来源，用于自由基接力。
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