1183403-48-6Relevant academic research and scientific papers
Copper-Catalyzed Amination of Congested and Functionalized α-Bromocarboxamides with either Amines or Ammonia at Room Temperature
Ishida, Syo,Takeuchi, Kentaro,Taniyama, Nobuhiro,Sunada, Yusuke,Nishikata, Takashi
, p. 11610 - 11614 (2017)
There are several reports on the synthesis of alkylamines, but most of the reported methods are not suitable for the synthesis of hindered amines. In this research, we found that a copper catalyst is effective for the formation of congested C?N bonds at room temperature. Control experiments revealed that a copper amide is a key intermediate. Moreover, when a chiral amine was used, a quaternary carbon stereogenic center was created with good selectivity.
Diamides conformationally restricted with central amino acid: Design, synthesis, and biological activities
Chen, Rui-Jia,Cheng, Jia-Gao,Dong, Le-Feng,Feng, Ting-Ting,Gu, Yu-Cheng,Li, Zhong,Shao, Xu-Sheng,Wang, Gang-Ao,Wang, Jun-Jie,Xu, Xiao-Yong,Xu, Zhi-Ping,Zhou, Cong
supporting information, (2022/02/03)
Diamide insecticides, represented by chlorantraniliprole (CHL), were widely applied in the control of lepidopteran insects. In efforts to develop bioactive diamides with novel scaffolds, we design and synthesized a series of diamides containing central amino acids to conformationally simulate CHL. Bioassay results indicated that most compounds containing 1-aminocyclopropane-1-carboxylic acid exhibited excellent larvacidal potency against Mythimna separate and Plutella xylostella. After a systematic structure–activity relationship study, 1–23 was identified as a potential insecticidal candidate with LC50 values of 34.920 mg·L?1 against M. separate and 61.992 mg·L?1 on P. xylostella. Finally, molecular docking revealed the possible binding mode of 1–23 with the target protein, ryanodine receptors.
