57372-14-2Relevant articles and documents
Design, synthesis and fungicidal activity evaluation of novel pyrimidinamine derivatives containing phenyl-thiazole/oxazole moiety
Yan, Zhongzhong,Liu, Aiping,Ou, Yingcan,Li, Jianming,Yi,Zhang, Ning,Liu, Minhua,Huang, Lu,Ren, Jianwei,Liu, Weidong,Hu, Aixi
, p. 3218 - 3228 (2019/06/05)
Diflumetorim is a member of pyrimidinamine fungicides that possess excellent antifungal activities. Nevertheless, as reported that the activity of diflumetorim to corn rust (Puccinia sorghi) was not ideal (EC50 = 53.26 mg/L). Herein, a series of novel pyrimidinamine derivatives containing phenyl-thiazole/oxazole moiety were designed based on our previous study and the structural characteristics of diflumetorim, synthesized and bioassayed to discover novel fungicides with excellent antifungal activities. Among these compounds, T18 gave the optimal fungicidal activity, which respectively offers control effects with EC50 values of 0.93 mg/L against P. sorghi and 1.24 mg/L against E. graminis, significantly superior to commercial fungicides diflumetorim, tebuconazole, and flusilazole. Cell cytotoxicity results suggested that compound T18 has lower toxicities than diflumetorim. Furthermore, DFT calculation indicated that the phenyl-thiazole/oxazole moiety plays an unarguable role in the improvement of activity, which will contribute to designing and developing more potent compounds in the future.
Synthesis of Heterocycle-fused Pyridine N-Oxides from Oximes and Diazo Compounds via RhIII-Catalyzed C-H Activation and Annulation
Sun, Peng,Wu, Youzhi,Yang, Tie,Wu, Xiaoming,Xu, Jinyi,Lin, Aijun,Yao, Hequan
supporting information, p. 2469 - 2473 (2015/08/18)
A RhIII-catalyzed tandem C-H activation and C-N bond formation reaction between oximes and diazo compounds for the synthesis of heterocycle-fused pyridine N-oxides has been developed. The reaction exhibits good functional group tolerance and regioselectivity. After simple transformation, the 1-substituted, 1,3-disubstituted, 1,4-disubstituted and 1,3,4-trisubstituted heterocycle-fused pyridines were all obtained in high efficiency. Moreover, this strategy has also been expanded to the synthesis of a key intermediate for the construction of one potential anti-HIV agent.