通过受阻（掩蔽）异氰酸酯的 Friedel-Crafts 环化反应合成吲唑酮。
Synthesis of Indazolones via Friedel-Crafts Cyclization of Blocked (Masked) N-Isocyanates.
机构信息
Centre for Catalysis Research and Innovation, Department of Chemistry and Biomolecular Sciences, University of Ottawa , 10 Marie-Curie, Ottawa, ON K1N 6N5, Canada.
Department of Organic Chemistry, Faculty of Pharmacy, Al-Azhar University , Cairo 11884, Egypt.
出版信息
J Org Chem. 2017 Sep 15;82(18):9890-9897. doi: 10.1021/acs.joc.7b01607. Epub 2017 Aug 31.
Nitrogen-substituted isocyanates (N-isocyanates) are rare amphoteric reagents with high, but underdeveloped synthetic potential. Herein, we study the formation of indazolones by Friedel-Crafts cyclization of N-isocyanates using blocked (masked) N-isocyanate precursors: the effect of the masking group and the reaction scope have been delineated. Substrate synthesis has also been improved using a reported copper-catalyzed coupling of arylbismuth(V) reagents that is compatible with the hemilabile OPh blocking group.
氮取代异氰酸酯（N-异氰酸酯）是一种罕见的两性试剂，具有很高的合成潜力，但尚未得到充分开发。在此，我们研究了使用封闭（掩蔽）N-异氰酸酯前体的 N-异氰酸酯的Friedel-Crafts 环化反应形成吲唑酮的过程：已经描述了掩蔽基团的影响和反应范围。使用与半配位 OPh 封闭基团兼容的报道的芳基双（V）铋试剂的铜催化偶联，也改进了底物的合成。
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