30020-98-5Relevant articles and documents
Regioselective 2-alkylation of indoles with α-bromo esters catalyzed by Pd/P,P=O system
Tian, Wei,Li, Bowen,Tian, Duanshuai,Tang, Wenjun
supporting information, p. 197 - 200 (2021/08/13)
A palladium-catalyzed 2-alkylation of indoles with α-bromo esters is developed by employing a P,P=O ligand. The method features excellent regioselectivities, mild reaction conditions, and good functional group compatibility. The employment of the P,P=O ligand as well as 4? molecular sieves were crucial for the success of the transformation. Mechanistic studies indicate the reaction proceed through a radical pathway.
C3-Arylation of indoles with aryl ketonesviaC-C/C-H activations
Dai, Hui-Xiong,Guo, Zi-Qiong,Ma, Biao,Wang, Xing,Wang, Zhen-Yu,Xu, Hui
supporting information, p. 9716 - 9719 (2021/09/30)
C3-Arylation of indoles with aryl ketones is accomplishedviapalladium-catalyzed ligand-promoted Ar-C(O) cleavage and subsequent C-H arylation of indole. Various (hetero)aryl ketones are compatible in this reaction, affording the corresponding 3-arylindoles in moderate to good yields. Further introduction of an indole moiety into the natural products desoxyestrone and evodiamine demonstrate the synthetic utility of this protocol.
Metal and Oxidant Free Construction of Substituted- and/or Polycyclic Indoles: A Useful Alternative to Bischler and Related Syntheses
De Crescentini, Lucia,Favi, Gianfranco,Mantellini, Fabio,Mari, Giacomo,Santeusanio, Stefania
supporting information, (2020/08/27)
A wide range of substituted indoles or polycyclic derivatives containing the indole core are easily accessible by acidic treatment of aromatic amines and 1,2-diaza-1,3-dienes. Unlike the related indole-Bischler synthesis, the regioselectivity of the method here reported is unique and predictable, the yields are generally good and also electron withdrawing substituted indoles are smoothly recovered.