Dipartimento di Scienze Fisiche e Chimiche, Università di L'Aquila, Via Vetoio-67010 Capitol(AQ), Italy.
Org Lett. 2013 Jun 7;15(11):2766-9. doi: 10.1021/ol401098b. Epub 2013 May 28.
A tandem gold(I)-catalyzed aminocylization/fluorination and a two-step, one-pot gold(III)-catalyzed cyclization/electrophilic fluorination provide a convenient and general method for the synthesis of 3,3-difluoro-2-substituted-3H-indoles in good yield under mild conditions. Extension of the procedure to the synthesis of 2-aryl-3-fluoro-1H-indoles is described. The reaction proceeds smoothly in green ethanol and does not require any base, acid, or N-protective group.
串联的金（I）催化的氨环化/氟化和两步、一锅的金（III）催化的环化/亲电氟化提供了一种在温和条件下方便且通用的方法，用于合成 3,3-二氟-2-取代-3H-吲哚，产率良好。该方法扩展到 2-芳基-3-氟-1H-吲哚的合成。反应在环保的乙醇中顺利进行，不需要任何碱、酸或 N-保护基。
