51062-15-8Relevant articles and documents
8-Hydroxyquinolin-2(1H)-one analogues as potential β2-agonists: Design, synthesis and activity study
Xing, Gang,Zhi, Zhengxing,Yi, Ce,Zou, Jitian,Jing, Xuefeng,Yiu-Ho Woo, Anthony,Lin, Bin,Pan, Li,Zhang, Yuyang,Cheng, Maosheng
, (2021/07/19)
β2-Agonists that bind to plasmalemmal β2-adrenoceptors causing cAMP accumulation are widely used as bronchodilators in chronic respiratory diseases. Here, we designed and synthesized a group of 8-hydroxyquinolin-2(1H)-one analogues and studied their β2-agonistic activities with a cellular cAMP assay. Compounds B05 and C08 were identified as potent (EC50 2-agonists among the compounds tested. They behaved as partial β2-agonists in non-overexpressed HEK293 cells, and possessed rapid smooth muscle relaxant actions and long duration of action in isolated guinea pig tracheal strip preparations. In summary, B05 and C08 are β2-agonists with potential applicability in chronic respiratory diseases.
Catalytic C(sp3)?H Arylation of Free Primary Amines with an exo Directing Group Generated In Situ
Xu, Yan,Young, Michael C.,Wang, Chengpeng,Magness, David M.,Dong, Guangbin
supporting information, p. 9084 - 9087 (2016/07/26)
Herein, we report the palladium-catalyzed direct arylation of unactivated aliphatic C?H bonds in free primary amines. This method takes advantage of an exo-imine-type directing group (DG) that can be generated and removed in situ. A range of unprotected aliphatic amines are suitable substrates, undergoing site-selective arylation at the γ-position. Methyl as well as cyclic and acyclic methylene groups can be activated. Furthermore, when aniline-derived substrates were used, preliminary success with δ-C?H arylation was achieved. The feasibility of using the DG component in a catalytic fashion was also demonstrated.
Hydrogenolysis of 3-methyl-4-phenylmethyl-5(2H)-isoxazolone derivatives: A reinvestigation
Batra, Sanjay,Seth, M,Bhaduri, A P
, p. 60 - 62 (2007/10/02)
Hydrogenolysis of 3-methyl-4-phenylmethyl-5(2H)-isoxazolone (2a) and its derivatives 2b-e, 5a-e, 6a-e and 9a,b have been carried out over Pd/C and Raney-nickel.The products have been isolated and characterized.The intermediate products of hydrogenolysis of 2b-e have been trapped and simultaneous cleavage of N - O and C - C bonds in 9a,b has been suggested to explain the formation of the hydrogenolysis products 10a,b and 3a,b.