- Regioselective N-1 and C-2 diacylation of 3-substituted indoles with arylglyoxal hydrates for the synthesis of indolyl diketones
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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.
- Pan, Dalong,Chu, Jinpeng,Gao, Xianrui,Wang, Cuiping,Meng, Qingtao,Chi, Haijun,Dong, Yan,Duan, Chunying,Zhang, Zhiqiang
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supporting information
p. 6998 - 7003
(2018/10/17)
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- Catalytic asymmetric Meerwein-Ponndorf-Verley reduction of glyoxylates induced by a chiral N,N′-dioxide/Y(OTf)3 complex
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An asymmetric Meerwein-Ponndorf-Verley (MPV) reduction of glyoxylates was for the first time accomplished via an N,N′-dioxide/Y(OTf)3 complex with aluminium alkoxide and molecular sieves (MSs) as crucial additives. A variety of optically active α-hydroxyesters were obtained with excellent results. A possible reaction mechanism was proposed based on the experiments.
- Wu, Wangbin,Zou, Sijia,Lin, Lili,Ji, Jie,Zhang, Yuheng,Ma, Baiwei,Liu, Xiaohua,Feng, Xiaoming
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supporting information
p. 3232 - 3235
(2017/03/20)
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- Synthesis and antitumor evaluation of 2,3-diarylbenzofuran derivatives on HeLa cells
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2,2-Dihydroxyarylethanones, readily prepared from the commercially available aromatic ethyl ketones, were reacted with resorcinol, 3-methoxyphenol or 2-methoxyphenol in multi steps one-pot manner promoted by trifluoroacetic acid to furnish the 2,3-diarylbenzofuran derivatives in 22–95% yield. Sixteen targeted compounds were synthesized and characterized by 1H NMR, 13C NMR and HRMS. MTT assay indicated that most compounds possessed effectively inhibitory activities against the proliferation of HeLa cell. Among them, 4f had the highest inhibitory activities, with the IC50 being 13.40?±?2.04?μmol/L. Cell cycle analysis, Annexin V-FITC/propidium iodide dual staining assay and western blotting analysis revealed that 4f inhibited the proliferation of Hela cell through apoptosis induction in a dose-dependent manner via obviously up-regulated the levels of Bak and Bim, while striking down-regulated the level of Bcl-2 and Bcl-xL protein.
- He, Guo-Xue,Yuan, Jing-Mei,Zhu, Hai-Miao,Wei, Kai,Wang, Ling-Yun,Kong, Shi-Lin,Mo, Dong-Liang,Pan, Cheng-Xue,Su, Gui-Fa
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supporting information
p. 1660 - 1664
(2017/04/04)
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- Naphthol synthesis: Annulation of nitrones with alkynes: Via rhodium(III)-catalyzed C-H activation
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An efficient and redox-neutral naphthol synthesis has been realized via rhodium(iii) catalyzed C-H activation of α-carbonyl nitrones and annulation with alkynes, where the nitrone group functioned as a traceless directing group.
- Wang, Qiang,Xu, Youwei,Yang, Xifa,Li, Yunyun,Li, Xingwei
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supporting information
p. 9640 - 9643
(2017/09/01)
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- Copper-Assisted Synthesis of 2-Hydroxyphenyl-1,2-diones from Phenols and 2-Oxoaldehydes
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An efficient copper(II)-catalyzed protocol for the ortho-functionalization of phenols was developed. A wide variety of 2-oxoaldehydes and phenols were tolerated, and the corresponding 2-hydroxyphenyl-1,2-diones were afforded in appreciable yields.
- Battini, Narsaiah,Battula, Satyanarayana,Ahmed, Qazi Naveed
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supporting information
p. 658 - 662
(2017/01/18)
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