A mild and readily scalable procedure for the N-1-difluoromethylation of ethyl 6-((tert-butyldiphenylsilyl)oxy)-1H-indazole-3-carboxylate and its applications to the N-difluoromethylation of indazole, benzotriazole, imidazole, indole and pyrazole derivatives

[Display omitted] •Mild condition.•Scalable.•Suitable for substartes bearing labile groups. A set of mild conditions for the N-1-difluoromethylation of ethyl 6-((tert-butyldiphenylsilyl)oxy)-1H-indazole-3-carboxylate (1) with chlorodifluoromethane (CHClF2) on large scale (up to 33 g) is described. A...

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Veröffentlicht in:	Journal of fluorine chemistry 2020-06, Vol.234, p.109514, Article 109514
Hauptverfasser:	Hong, Zhenqiu, Hou, Xiaoping, Zhao, Rulin, Li, Jianqing, Pawluczyk, Joseph, Wang, Bei, Kempson, James, Khandelwal, Purnima, Smith, Leon M., Glunz, Peter, Mathur, Arvind
Format:	Artikel
Sprache:	eng
Schlagworte:	18-crown-6 ether Benzotriazole Chlorodifluoromethane Derivatives High temperature Imidazole Indazole Indoles N-1-difluoromethylation NaI Pyrazole
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