6-SF-吲哚唑的合成及甘美唑的 SF-类似物。
Synthesis of 6-SF-indazoles and an SF-analog of gamendazole.
机构信息
Department of Chemistry, PO Box 117200, University of Florida, Gainesville, FL 32611-7200, USA.
出版信息
Org Biomol Chem. 2018 Aug 15;16(32):5793-5799. doi: 10.1039/c8ob01460d.
This work describes an efficient synthetic approach for a new type of SF5-substituted heterocyclic system, namely 6-SF5-indazoles. During this study, various derivatives of 6-SF5-indazoles such as bromo, iodo, nitro, N-acetyl and N-benzyl substituted compounds were synthesized and characterized. In addition, the utility of the synthetic methodology was demonstrated via the synthesis of 6-SF5-gamendazole - a fully matched analog of the experimental male contraceptive gamendazole, which has a 6-CF3-substituted indazole core.
这项工作描述了一种新型 SF5 取代杂环系统，即 6-SF5-吲哚的有效合成方法。在这项研究中，合成并表征了各种 6-SF5-吲哚的衍生物，如溴代、碘代、硝基、N-乙酰基和 N-苄基取代化合物。此外，通过合成 6-SF5-孕二烯唑（实验性男性避孕药孕二烯唑的完全匹配类似物），展示了该合成方法的实用性，其核心为 6-CF3 取代的吲哚。
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