Fluorinated motifs are prevalent in both pharmaceuticals and agrochemicals.The incorporation of fluorine-containing moieties to drug candidates has emerged as a potent strategy for lead optimization in pharmaceutical ...Fluorinated motifs are prevalent in both pharmaceuticals and agrochemicals.The incorporation of fluorine-containing moieties to drug candidates has emerged as a potent strategy for lead optimization in pharmaceutical research and development.While extensive research has been devoted to constructing molecules that incorporate a trifluoromethylthio(SCF_(3)−)group on a stereogenic carbon,the synthesis of trifluoromethylthiolated alkanes featuring a SCF_(3)-substituted stereogenic carbon at non-activated site remains understudied.Herein,we report a Cu-catalyzed regio-and enantioselective hydroallylation of 1-trifluoromethylthiolated alkenes.Important to the process is the regio-and enantioselective Cu-H insertion to SCF_(3)-substituted alkene to form chiralα-SCF_(3) alkyl copper intermediates,outcompeting unproductive insertion to the coupling partner,and eventually proceed to afford optically active homoallylic trifluoromethylthiolated products.展开更多
A visible-light-induced spirocyclizative hydroarylation via reductive dearomatization of a series of non activated arenes including 2-phenyl indoles and naphthalene derivatives under mild conditions is de scribed.An i...A visible-light-induced spirocyclizative hydroarylation via reductive dearomatization of a series of non activated arenes including 2-phenyl indoles and naphthalene derivatives under mild conditions is de scribed.An intriguing chemoselective dearomative hydroarylation of 2-phenyl indoles is presented.Th dearomative hydroarylation protocol rapidly delivers valuable spirocycles with carbon-carbon doub bonds from readily accessible aromatic precursors in a single step.展开更多
In this study,we report a palladium-catalyzed carbene C-H insertion reaction of non-activated arenes using N-tosylhydrazones as both carbene and olefin precursors.This method consists of a two-step,one-pot process,whe...In this study,we report a palladium-catalyzed carbene C-H insertion reaction of non-activated arenes using N-tosylhydrazones as both carbene and olefin precursors.This method consists of a two-step,one-pot process,where the arenes are first thianthrenated and then undergo migratory insertion/β-H elimination with N-tosylhydrazones to form aryl alkenes.This highly site-selective C-H alkenylation of arenes demonstrates a relatively broad substrate scope and exhibits high tolerance for halogen substituents.Importantly,this transformation allows for the modification of the arene moiety in commercially available bioactive molecules,underscoring its significant potential for late-stage functionalization of arenecontaining pharmaceuticals.展开更多
This work was on non-activated and activated lateritic soil used in proportions of 0%to 30%,to replace fine sand by wt.%,in the production of lateritic concrete.A mix of 1:2:4 was used,and the cube samples were cured...This work was on non-activated and activated lateritic soil used in proportions of 0%to 30%,to replace fine sand by wt.%,in the production of lateritic concrete.A mix of 1:2:4 was used,and the cube samples were cured in four(4)curing media of water,sand,polythene,and sawdust.The aim was to evaluate the effects of these curing methods on the mechanical strengths,and other properties of lateritic concrete.The sensitivity of the generated data was characterized statistically and developing linear regression models for predictions.For the Non-Activated Laterite soil(NALS,control mix(0%)),the design strength of 20 MPa was achieved by all the curing methods(standard and non-standard).However,for other replacement levels,water curing was adequate for 10%and 30%,sand at 10%,and sawdust for 20%and 30%,respectively.On the other hand,for the Activated Laterite soil(ALS),the 20 MPa design strength was met only at 0%replacement for all curing methods.Sawdust medium at 10%also satisfied the 20 MPa strength.展开更多
基金the National Key R&D Program of China(No.2021YFF0701700)the National Natural Science Foundation of China(Nos.22271264 and 21971228)for financial support.
文摘Fluorinated motifs are prevalent in both pharmaceuticals and agrochemicals.The incorporation of fluorine-containing moieties to drug candidates has emerged as a potent strategy for lead optimization in pharmaceutical research and development.While extensive research has been devoted to constructing molecules that incorporate a trifluoromethylthio(SCF_(3)−)group on a stereogenic carbon,the synthesis of trifluoromethylthiolated alkanes featuring a SCF_(3)-substituted stereogenic carbon at non-activated site remains understudied.Herein,we report a Cu-catalyzed regio-and enantioselective hydroallylation of 1-trifluoromethylthiolated alkenes.Important to the process is the regio-and enantioselective Cu-H insertion to SCF_(3)-substituted alkene to form chiralα-SCF_(3) alkyl copper intermediates,outcompeting unproductive insertion to the coupling partner,and eventually proceed to afford optically active homoallylic trifluoromethylthiolated products.
基金the financial supports from the National Natural Science Foundation of China(Nos.22022111,21871257,21801240)the Natural Science Foundation of Fujian Province(No.2020J02008)the Strategic Priority Research Program of the Chinese Academy of Sciences(No.XDB20000000)。
文摘A visible-light-induced spirocyclizative hydroarylation via reductive dearomatization of a series of non activated arenes including 2-phenyl indoles and naphthalene derivatives under mild conditions is de scribed.An intriguing chemoselective dearomative hydroarylation of 2-phenyl indoles is presented.Th dearomative hydroarylation protocol rapidly delivers valuable spirocycles with carbon-carbon doub bonds from readily accessible aromatic precursors in a single step.
基金the Natural Science Foundation of Guangdong Province(Nos.2021A1515010186,2022A1515010744)Guangdong Provincial Key Laboratory of Construction Foundation(No.2023B1212060022)for the financial support。
文摘In this study,we report a palladium-catalyzed carbene C-H insertion reaction of non-activated arenes using N-tosylhydrazones as both carbene and olefin precursors.This method consists of a two-step,one-pot process,where the arenes are first thianthrenated and then undergo migratory insertion/β-H elimination with N-tosylhydrazones to form aryl alkenes.This highly site-selective C-H alkenylation of arenes demonstrates a relatively broad substrate scope and exhibits high tolerance for halogen substituents.Importantly,this transformation allows for the modification of the arene moiety in commercially available bioactive molecules,underscoring its significant potential for late-stage functionalization of arenecontaining pharmaceuticals.
文摘This work was on non-activated and activated lateritic soil used in proportions of 0%to 30%,to replace fine sand by wt.%,in the production of lateritic concrete.A mix of 1:2:4 was used,and the cube samples were cured in four(4)curing media of water,sand,polythene,and sawdust.The aim was to evaluate the effects of these curing methods on the mechanical strengths,and other properties of lateritic concrete.The sensitivity of the generated data was characterized statistically and developing linear regression models for predictions.For the Non-Activated Laterite soil(NALS,control mix(0%)),the design strength of 20 MPa was achieved by all the curing methods(standard and non-standard).However,for other replacement levels,water curing was adequate for 10%and 30%,sand at 10%,and sawdust for 20%and 30%,respectively.On the other hand,for the Activated Laterite soil(ALS),the 20 MPa design strength was met only at 0%replacement for all curing methods.Sawdust medium at 10%also satisfied the 20 MPa strength.
