119225-94-4Relevant academic research and scientific papers
Copper-Catalyzed Selective 1,2-Difunctionalization of N-Heteroaromatics through Cascade C-N/CC/CO Bond Formation
He, Qianlin,Xie, Feng,Xia, Chuanjiang,Liang, Wanyi,Guo, Ziyin,Zhu, Zhongzhi,Li, Yibiao,Chen, Xiuwen
, p. 7976 - 7980 (2020)
This study presents an efficient strategy for constructing 1,2-difunctionalized quinoline derivatives via the multicomponent cascade coupling of N-heteroaromatics with alkyl halides and different terminal alkynes. This reaction was achieved through sequential functionalization at the one- and two-positions of quinolines, which displayed a broad substrate scope, environmental friendliness, excellent functional group tolerance, high atom efficiency, and chemoselectivity. The multicomponent coupling involved the abnormal construction of new C-N, CC, and CO bonds in one pot. The applicability of this method was further demonstrated by the late-stage functionalization of complex drug molecules under the established conditions.
1,2-substituted quinoline compound as well as preparation method and application thereof
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Paragraph 0073-0078, (2020/12/15)
The invention discloses a 1,2-substituted quinoline compound as well as a preparation method and application thereof. The compound has a structure shown in the formula defined in the specification, wherein R1 comprises substituted or unsubstituted alkyl, substituted or unsubstituted ester group, substituted or unsubstituted heterocyclic aryl and substituted or unsubstituted steroid ring group, R2comprises alkyl, R3 comprises at least one of hydrogen, alkyl or aromatic hydrocarbon oxy, and X and Y are respectively and independently selected from C or N. The compound provided by the scheme of the invention has good anti-tumor activity, and has a good inhibition effect on tumor cells such as human leukemia cells K562, human promyelocytic acute leukemia cells HL60 and human cervical cancer Hela cells. Therefore, the compound can be used as an anti-tumor reagent for in-vitro anti-tumor activity screening, and can also be used in drugs for preventing and treating tumors.
