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Direct Synthesis of 4-Aryl-1,2,3-triazoles via I2-Promoted Cyclization under Metal- and Azide-Free Conditions
The Journal of Organic Chemistry ( IF 3.6 ) Pub Date : 2021-09-14 , DOI: 10.1021/acs.joc.1c01702
Chun Huang 1 , Xiao Geng 2 , Peng Zhao 1 , You Zhou 1 , Xiao-Xiao Yu 1 , Li-Sheng Wang 1 , Yan-Dong Wu 1 , An-Xin Wu 1
Affiliation  

We herein report an iodine-mediated formal [2 + 2 + 1] cyclization of methyl ketones, p-toluenesulfonyl hydrazines, and 1-aminopyridinium iodide for preparation of 4-aryl-NH-1,2,3-triazoles under metal- and azide-free conditions. Notably, this is achieved using p-toluenesulfonyl hydrazines and 1-aminopyridinium iodide as azide surrogates, providing a novel route toNH-1,2,3-triazoles. Furthermore, this approach provides rapid and practical access to potent inhibitors of indoleamine 2,3-dioxygenase (IDO).

中文翻译:

在无金属和无叠氮化物条件下通过 I2 促进环化直接合成 4-Aryl-1,2,3-三唑

本文我们报告碘介导的正式[2 + 2 + 1]甲基酮,环化p甲苯磺酰肼,和1-氨基吡啶碘化物用于制备4-芳基- NH下金属-1,2,3-三唑和无叠氮化物条件。值得注意的是,这是使用甲苯磺酰肼和碘化 1-氨基吡啶鎓作为叠氮化物替代物实现的,为NH -1,2,3-三唑提供了一条新途径。此外,这种方法提供了对吲哚胺 2,3-双加氧酶 (IDO) 的强效抑制剂的快速且实用的途径。
更新日期:2021-10-01
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