钯催化的4-芳基-吡咯并[2,3 -]嘧啶的芳烃C-H氟烷氧基化反应的位点选择性
Palladium-catalysed site-selective arene C-H fluoroalkoxylation of 4-aryl-pyrrolo[2,3-]pyrimidines.
作者信息
Jiang Yunfeng, Pan Chenhong, Tang Ting, Liu Mingrui, Zhang Xingxian
机构信息
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, P. R. China.
School of Public Health, Hangzhou Normal University, Hangzhou 311121, P. R. China.
出版信息
Org Biomol Chem. 2023 Mar 29;21(13):2748-2753. doi: 10.1039/d3ob00084b.
A palladium-catalysed direct arene C-H fluoroalkoxylation of 4-aryl-pyrrolo[2,3-]pyrimidine derivatives with fluorinated alcohols is described. Highly site-selective mono- or bis-fluoroalkoxylation can be achieved by tuning the reaction conditions, affording various fluoroalkoxylated pyrrolo[2,3-]pyrimidine derivatives in moderate to good yields, which offer rational tailoring of their biological activity for their application in the field of pharmaceutical chemistry.
本文描述了一种钯催化的4-芳基-吡咯并[2,3 -]嘧啶衍生物与氟化醇的直接芳烃C-H氟烷氧基化反应。通过调节反应条件可实现高度的位点选择性单氟烷氧基化或双氟烷氧基化，以中等至良好的产率得到各种氟烷氧基化的吡咯并[2,3 -]嘧啶衍生物，这为在药物化学领域应用中合理调整其生物活性提供了可能。
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