1476035-07-0Relevant academic research and scientific papers
Regioselective N-1 and C-2 diacylation of 3-substituted indoles with arylglyoxal hydrates for the synthesis of indolyl diketones
Pan, Dalong,Chu, Jinpeng,Gao, Xianrui,Wang, Cuiping,Meng, Qingtao,Chi, Haijun,Dong, Yan,Duan, Chunying,Zhang, Zhiqiang
, p. 6998 - 7003 (2018)
A highly regioselective N-1 and C-2 diacylation of 3-substituted indoles with arylglyoxal hydrates to afford N-1 and C-2 indolyl diketones in moderate to good yields is described. Notably, the control of regioselectivity is achieved by small changes in the Cu catalyst, additive and solvent. Importantly, the intermediates for N-1 and C-2 diacylation were detected and two plausible pathways were also proposed.
1-aryl-2 - (3-methyl-2-indolyl) - 1,2-ethylene-diketone derivative synthesis method
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Paragraph 0028-0031, (2017/01/26)
The invention discloses a synthetic method of a 1-aryl-2-(3-methyl-2-indolyl)-1, 2-ethyl diketone derivative, wherein a target product can be directly prepared in an organic solvent. The method comprises the following step: by using 3-methylindole (II) and an R1 (R2)-substituted phenylglyoxal hydrate (III) as a raw material, carrying out an acylation reaction in an organic solvent at 60-140 DEG C for 6-9 hours to obtain a reaction liquid of the 1-aryl-2-(3-methyl-2-indolyl)-1, 2-ethyl diketone derivative (I), wherein the reaction formula is shown in the specification. According to the method disclosed by the invention, no metal catalysts are required and in the organic solvent, the R1 (R2)-substituted phenylglyoxal hydrate is an acylation reagent which is directly acylation-reacted with 3-methylindole. The system is free from other oxidizing agents or additives and the method is relatively mild in reaction conditions, good in selectivity, high in yield and low in cost.
Palladium-catalyzed synthesis of 3-acylated indoles involving oxidative cross-coupling of indoles with α-amino carbonyl compounds
Tang, Ri-Yuan,Guo, Xiao-Kang,Xiang, Jian-Nan,Li, Jin-Heng
, p. 11163 - 11171 (2013/12/04)
A new and selective C-N bond oxidative cleavage method to 3-acylated indoles by Pd-catalyzed oxidative cross coupling of indoles with α-amino carbonyl compounds has been developed; moreover, one-pot synthesis of 3-acylated indoles from 2-ethynylanilines and α-amino carbonyl compounds has also been established. Importantly, the products 3-acylated indoles can be used to construct polyheterocyclic compound, which can be employed as efficient probes for Hg2+ and Fe3+.
