16576-28-6Relevant articles and documents
Copper(i)-catalyzed tandem synthesis of 2-acylquinolines from 2-ethynylanilines and glyoxals
Chu, Xiaoxiao,Jia, Jian,Liu, Gang,Liu, Xiguang,Wang, Guanghui,Yu, Mingwu,Zhao, Ximei
, p. 11811 - 11814 (2021/11/30)
An efficient one-step synthesis of 2-acylquinolines using a copper-catalyzed tandem reaction of 2-ethynylanilines with glyoxals in the presence of piperidine has been developed. This new protocol successfully avoids multi-step operation and the use of highly toxic cyanides required in traditional methods, and provides a practical tool for synthetic and pharmaceutical chemists. Various 2-acylquinolines are obtained with perfect regioselectivity in moderate to good yields (up to 86%). The potential synthetic utility of this method is exemplified by a large-scale experiment and synthetic transformation of the products.
Rhodium-Catalyzed Pyridine N-Oxide Assisted Suzuki-Miyaura Coupling Reaction via C(O)-C Bond Activation
Zhong, Jing,Long, Yang,Yan, Xufei,He, Shiyu,Ye, Runyou,Xiang, Haifeng,Zhou, Xiangge
, p. 9790 - 9794 (2019/12/24)
A rhodium-catalyzed Suzuki-Miyaura coupling reaction via C(O)-C bond activation to form 2-benzoylpyridine N-oxide derivatives is reported. Both the C(O)-C(sp2) and C(O)-C(sp3) bond could be activated during the reaction with yields up to 92%. The N-oxide moiety could be employed as a traceless directing group, leading to free pyridine ketones.
AROYLQUINOLINE COMPOUNDS
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Page/Page column 11, (2011/11/13)
A serious of nitro heterocyclic derivatives including a structure of formula (I) are provided. In formula (I), P, Q and R1 to R8 are defined in the specification. The derivatives disclosed in the present invention are characterized in inhibiting tubulin p
5-Amino-2-Aroylquinolines as highly potent tubulin polymerization inhibitors
Nien, Chih-Ying,Chen, Yun-Ching,Kuo, Ching-Chuan,Hsieh, Hsing-Pang,Chang, Chi-Yen,Wu, Jian-Sung,Wu, Su-Ying,Liou, Jing-Ping,Chang, Jang-Yang
supporting information; experimental part, p. 2309 - 2313 (2010/08/07)
A series of aroylquinoline derivatives were synthesized and evaluated for anticancer activity. 5-Amino6-methoxy-2-aroylquinoline 15 showed more potent antiproliferative activity (IC50 values ranging from 0.2 to 0.4 nM) as compared to la (combretastatin A-4) (IC50 = 1-9-835 nM) against various human cancer cell lines and a MDR-resistant cancer cell line. Compound 15 (IC50 = 1-6 μM) exhibited more potent inhibition of tubulin polymerization than la (IC50 = 2.1 μM) and showed strong binding property to the colchicine binding site of microtubules.
