Ji Jian, Guan Cong, Wei Qinghua, Chen Xuwen, Zhao Yun, Liu Shunying
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, 200062, China.
Org Lett. 2022 Jan 14;24(1):132-136. doi: 10.1021/acs.orglett.1c03743. Epub 2021 Dec 20.
We developed a highly regioselective base-induced synthesis of -substituted 1,2,3-triazoles from -sulfonyl-1,2,3-triazoles and alkyl bromides/alkyl iodides at room temperature. We propose an S2-like mechanistic pathway to explain the high -regioselectivity. The protocol features a broad substrate scope and generates products in good to excellent yields (72-90%).
我们开发了一种在室温下由β-磺酰基-1,2,3-三唑与溴代烷/碘代烷通过碱诱导进行的高度区域选择性合成α-取代的1,2,3-三唑的方法。我们提出了一种类似S2的机理途径来解释这种高区域选择性。该方法具有广泛的底物范围，并且能以良好至优异的产率（72-90%）生成产物。
