Regioselective C-H Alkynylation with Haloalkynes Enabled by Nitrogen Functionality

IF 4.6 1区化学 Q1 CHEMISTRY, ORGANIC

Organic Chemistry Frontiers Pub Date : 2025-04-26 DOI:10.1039/d5qo00578g

Qiaoya Zhang, Bifu Liu, Ci Chen, Yinling Li, Kejun Feng, Sheng Hu, Yang Gao, Yanping Huo, Qian Chen, Xianwei Li

引用次数: 0

Abstract

Regioselective introduction of versatile alkyne functionality would enable rapid construction of molecular complexity, however, steric hindered silyl-contained alkynylation reagents were typically required, and thus, hampered the further applications. Herein, we developed transformable nitrogen functionality enabled regioselective C‒H alkynylation cascade with aliphatic haloalkynes, furnishing alkynes and heterocycles, which thus facilitated concise delivery of CB2 receptor agonist, protein kinase inhibitor analogues.

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氮官能团激活的C-H与卤代烷的区域选择性烷基化

区域选择性引入多功能化炔可以快速构建复杂分子，然而，通常需要空间位阻的含硅烷基烷基化试剂，因此，阻碍了进一步的应用。在此，我们开发了可转换的氮功能，使C-H炔基化与脂肪族卤代炔、供给炔和杂环级联，从而促进了CB2受体激动剂、蛋白激酶抑制剂类似物的简明传递。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Organic Chemistry Frontiers CHEMISTRY, ORGANIC-

CiteScore

7.90

自引率

11.10%

发文量

686

审稿时长

1 months

期刊介绍： Organic Chemistry Frontiers is an esteemed journal that publishes high-quality research across the field of organic chemistry. It places a significant emphasis on studies that contribute substantially to the field by introducing new or significantly improved protocols and methodologies. The journal covers a wide array of topics which include, but are not limited to, organic synthesis, the development of synthetic methodologies, catalysis, natural products, functional organic materials, supramolecular and macromolecular chemistry, as well as physical and computational organic chemistry.