104-97-2Relevant articles and documents
Synthesis and Evaluation of 1,3,4-Thiadiazole Derivatives Containing Cyclopentylpropionamide as Potential Antibacterial Agent
Zhang, Min,Xu, Weiming,Wei, Kun,Liu, Hongwu,Yang, Qin,Liu, Qin,Yang, Liyun,Luo, Yuqin,Xue, Wei
, (2019)
This study aimed to identify new strategies for the control of these plant bacterial diseases by combining a pharmacophoric group of different bioactive compounds. A series of 3-cyclopentylpropionamide containing 1,3,4-thiadiazole derivatives was synthesized and characterized via 1H-NMR, 13C-NMR, and HRMS. Bioassay results indicated that compounds 7a, 7d, 7j, 7m, 7n, and 7s had excellent antibacterial activity compared with the positive control. Among them, compound 7a exhibited remarkable inhibitory effect against Xoo with an EC50 of 21.41?μg/mL, which surpassed that of thiodiazole copper (67.71?μg/mL) and bismerthiazol (69.05?μg/mL). Greenhouse condition tests further revealed that 7a had approximately equal curative activity and better protection activity (41.58%) against bacterial leaf blight of rice than that of thiodiazole copper and bismerthiazol (46.86 and 42.25%, respectively). Structure–activity relationship analysis exhibited that sulfone fragment favored inhibition. Overall, this study suggested that derivatives containing 1,3,4-thiadiazole 3-cyclopentylpropanamide can be used as new lead compounds for bactericide studies.
Design and Synthesis of 2-Methyl-7-aminobenzoxazole as Auxiliary in the Palladium(II)-Catalyzed Arylation of a beta-Positioned C(sp3)-H Bond
Luo, Feihua,Yang, Jun,Li, Zhengkai,Xiang, Haifeng,Zhou, Xiangge
, p. 887 - 893 (2016)
A palladium(II)-catalyzed direct arylation of methylene C(sp3)-H bonds by 2-methyl-7-aminobenzoxazole as an effective auxiliary is reported. This process exhibited high beta-site selectivity, broad substrate scope, and compatibility with different functional groups with moderate to high yields up to 89%.
Remote Directed Isocyanation of Unactivated C(sp3)-H Bonds: Forging Seven-Membered Cyclic Ureas Enabled by Copper Catalysis
Zhang, Hongwei,Tian, Peiyuan,Ma, Lishuang,Zhou, Yulu,Jiang, Cuiyu,Lin, Xufeng,Xiao, Xiao
supporting information, p. 997 - 1002 (2020/02/15)
Reported herein is an unprecedented copper-catalyzed site-selective ?-C(sp3)-H bonds activation of aliphatic sulfonamides for constructing the synthetically useful seven-membered N-heterocycles. A key to success is the use of in-situ-formed amide radicals, to activate the inert C(sp3)-H bond, and inexpensive TMSNCO, as a coupling reagent under mild conditions. To the best of our knowledge, this represents the first use of alkylamine derivatives as a five-membered synthon to prepare a seven-membered N-heterocycles.