Atropisomeric anilides are one of important C-N axially chiral compounds.Compared with the A/-terminal functionalization to prepare such compounds,C-terminal functionalization strategies have been rarely reported.We d...Atropisomeric anilides are one of important C-N axially chiral compounds.Compared with the A/-terminal functionalization to prepare such compounds,C-terminal functionalization strategies have been rarely reported.We describe herein an efficient synthesis of axially chiral anilides enabled by Pd-catalyzed desymmetric Sonogashira cross-coupling reactions with the use of a newly identified Ming-Phos.Moderate to high yields with high enantioselectivities(up to 98%ee)were obtained.展开更多
Metalaxyl is an anilide pesticide that is widely used to control plant diseases caused by Peronosporales species.In order to study the toxic effects,zebrafish embryos were exposed to metalaxyl at nominal concentration...Metalaxyl is an anilide pesticide that is widely used to control plant diseases caused by Peronosporales species.In order to study the toxic effects,zebrafish embryos were exposed to metalaxyl at nominal concentrations of 5,50 and 500 ng/L for 72 hr,and the cardiac development and functioning of larvae were observed.The results showed that metalaxyl exposure resulted in increased rates of pericardial edema,heart hemorrhage and cardiac malformation.The distance between the sinus venosus and bulbus arteriosus,stroke volume,cardiac output and heart rate were significantly increased in larvae exposed to 50 and 500 ng/L metalaxyl compared to solvent control larvae.Significant upregulation in the transcription of tbx5,gata4 and myh6 was observed in the 50 and 500 ng/L treatments,and that of nkx2.5 and myl7 was observed in the 5,50 and 500 ng/L groups.These disturbances may be related to cardiac developmental and functional defects in the larvae.The activity of Na+/K+-ATPase and Ca2+-ATPase was significantly increased in zebrafish embryos exposed to 500 ng/L metalaxyl,and the mRNA levels of genes related to ATPase (atp2a11,atp1b2b,and atp1a3b)(in the 50 and 500 ng/L groups) and calcium channels (cacna1ab)(in the 500 ng/L group) were significantly downregulated;these changes might be associated with heart arrhythmia and functional failure.展开更多
基金the funding support of NSFC(Nos.22031004,21921003,21901043)Shanghai Municipal Education Commission(No.20212308).
文摘Atropisomeric anilides are one of important C-N axially chiral compounds.Compared with the A/-terminal functionalization to prepare such compounds,C-terminal functionalization strategies have been rarely reported.We describe herein an efficient synthesis of axially chiral anilides enabled by Pd-catalyzed desymmetric Sonogashira cross-coupling reactions with the use of a newly identified Ming-Phos.Moderate to high yields with high enantioselectivities(up to 98%ee)were obtained.
基金supported by the National Natural Science Foundation of China(No.41376118)
文摘Metalaxyl is an anilide pesticide that is widely used to control plant diseases caused by Peronosporales species.In order to study the toxic effects,zebrafish embryos were exposed to metalaxyl at nominal concentrations of 5,50 and 500 ng/L for 72 hr,and the cardiac development and functioning of larvae were observed.The results showed that metalaxyl exposure resulted in increased rates of pericardial edema,heart hemorrhage and cardiac malformation.The distance between the sinus venosus and bulbus arteriosus,stroke volume,cardiac output and heart rate were significantly increased in larvae exposed to 50 and 500 ng/L metalaxyl compared to solvent control larvae.Significant upregulation in the transcription of tbx5,gata4 and myh6 was observed in the 50 and 500 ng/L treatments,and that of nkx2.5 and myl7 was observed in the 5,50 and 500 ng/L groups.These disturbances may be related to cardiac developmental and functional defects in the larvae.The activity of Na+/K+-ATPase and Ca2+-ATPase was significantly increased in zebrafish embryos exposed to 500 ng/L metalaxyl,and the mRNA levels of genes related to ATPase (atp2a11,atp1b2b,and atp1a3b)(in the 50 and 500 ng/L groups) and calcium channels (cacna1ab)(in the 500 ng/L group) were significantly downregulated;these changes might be associated with heart arrhythmia and functional failure.
