The Reaction of arylatrloxythiophosphoric hydrazide 2a～2d with glycosyl isothiocyanates 3a～3d gave the corresponding aryl N-（glycosylthioureylene）-arylthiophosphoramidates 4a～4d,5a～5d,6a～6d,7a～7d.The resulted ...The Reaction of arylatrloxythiophosphoric hydrazide 2a～2d with glycosyl isothiocyanates 3a～3d gave the corresponding aryl N-（glycosylthioureylene）-arylthiophosphoramidates 4a～4d,5a～5d,6a～6d,7a～7d.The resulted compounds contained glycosylthioureylene and thiophosphoric amide fragments.The glycosyl isothiocyanates 3a～3d were prepared by the reaction of α-D-glycosyl bromides with Pb（SCN）2.The biologic activities of the representative compounds were studied.展开更多
In searching for effective anticonvulsant agents,fourteen 6-aryl-4.5-di- hydro-3(2H)pyridazinones.fifteen 6-aryl-3(2H)pyridazinones,and seventeen 3-GABA derivatives of 6-aryIpyridazines have been synthesized,and evalu...In searching for effective anticonvulsant agents,fourteen 6-aryl-4.5-di- hydro-3(2H)pyridazinones.fifteen 6-aryl-3(2H)pyridazinones,and seventeen 3-GABA derivatives of 6-aryIpyridazines have been synthesized,and evaluated in mice for the ability to antagonize maximal electroshock seizure(MES).The ED_(50) values showed that 6-(2′,4′- dichlorophenyt)-3(2H)pyridazinone was the most potent anticonvulsant among these corn- pounds(ED_(50)=10.15 mg/kg).The structure-activity relationships of the aryl pyridazinones were studied.The result showed that:(1)the higher the value of the hydrophobic parameter л of the substituent on the phenyl ring.the more potent the anticonvulsant activity of the corn- pound.and(2)only the compounds with an electron withdrawing substituent on the phenyl ring exhibited appreciable anticonvulsant activity.展开更多
An efficient Cu catalyzed selective arylation/annulation cascade reaction of 2-alkynylanilines with diaryliodonium salts was developed.This reaction was selective to N-arylation instead of C-arylation,which provides a...An efficient Cu catalyzed selective arylation/annulation cascade reaction of 2-alkynylanilines with diaryliodonium salts was developed.This reaction was selective to N-arylation instead of C-arylation,which provides a simple synthetic method for N-aryl indoles.展开更多
Oxidative coupling of α-bromoarylacetonitriles and oxidative decyanation of diarylacetonitriles are efficiently realized by solid-liquid phase transfer catalysis using anhydrous K 3 PO 4 as base and TBAB as catalyst ...Oxidative coupling of α-bromoarylacetonitriles and oxidative decyanation of diarylacetonitriles are efficiently realized by solid-liquid phase transfer catalysis using anhydrous K 3 PO 4 as base and TBAB as catalyst in acetone at room temperature. In this mild and convenient method, α,β-dicyanostilbenes and diarylketones were prepared in good to excellent yields.展开更多
An efficient approach for the synthesis of N-arylated amides was developed via copper(Ⅱ) triflate-catalyzed direct oxidation of(aryl)methylamines to primary arylamides by air and subsequent N-arylation by diaryliodon...An efficient approach for the synthesis of N-arylated amides was developed via copper(Ⅱ) triflate-catalyzed direct oxidation of(aryl)methylamines to primary arylamides by air and subsequent N-arylation by diaryliodonium salts. Various substituted benzylamines could be applied in the reaction, providing a series of N-arylated amides in moderate to good yields. This method showed convenient, practical, and environment friendly advantages.展开更多
Synthesis of organosilanes from alkenes is a very important topic owing to their wide applications.A Ni/Cu dual metal-catalyzed arylsilylation of terminal alkenes,featuring migratory selectivity,has been developed.A w...Synthesis of organosilanes from alkenes is a very important topic owing to their wide applications.A Ni/Cu dual metal-catalyzed arylsilylation of terminal alkenes,featuring migratory selectivity,has been developed.A wide diversity of aliphatic silanes have been prepared from terminal alkenes,aryl halides and Suginome’s reagent.This protocol is highlighted by excellent regioselectivity,mild reaction conditions and good functional group tolerance.In addition to benzylic positions,carbon–carbon bonds can also be constructed at allylic positions.Preliminary mechanistic studies suggest that the copper cocatalyst promotes the transmetalation of Suginome’s reagent,and the addition of a Pyr Ox ligand inhibits the formation of side-products from the carbon-Heck pathway.Moreover,studies toward the nature of the Pyr Ox ligand revealed that the steric hindrance of the oxazoline moiety greatly affects the chain–walking process,but not the arylation step.展开更多
文摘The Reaction of arylatrloxythiophosphoric hydrazide 2a～2d with glycosyl isothiocyanates 3a～3d gave the corresponding aryl N-（glycosylthioureylene）-arylthiophosphoramidates 4a～4d,5a～5d,6a～6d,7a～7d.The resulted compounds contained glycosylthioureylene and thiophosphoric amide fragments.The glycosyl isothiocyanates 3a～3d were prepared by the reaction of α-D-glycosyl bromides with Pb（SCN）2.The biologic activities of the representative compounds were studied.
文摘In searching for effective anticonvulsant agents,fourteen 6-aryl-4.5-di- hydro-3(2H)pyridazinones.fifteen 6-aryl-3(2H)pyridazinones,and seventeen 3-GABA derivatives of 6-aryIpyridazines have been synthesized,and evaluated in mice for the ability to antagonize maximal electroshock seizure(MES).The ED_(50) values showed that 6-(2′,4′- dichlorophenyt)-3(2H)pyridazinone was the most potent anticonvulsant among these corn- pounds(ED_(50)=10.15 mg/kg).The structure-activity relationships of the aryl pyridazinones were studied.The result showed that:(1)the higher the value of the hydrophobic parameter л of the substituent on the phenyl ring.the more potent the anticonvulsant activity of the corn- pound.and(2)only the compounds with an electron withdrawing substituent on the phenyl ring exhibited appreciable anticonvulsant activity.
基金supported by the Intercollegiate Key Scientific Research Projects of Henan Province(15A150018)~~
文摘An efficient Cu catalyzed selective arylation/annulation cascade reaction of 2-alkynylanilines with diaryliodonium salts was developed.This reaction was selective to N-arylation instead of C-arylation,which provides a simple synthetic method for N-aryl indoles.
基金Natural Science Foundation of China (Grant No.NSFC 20672009)
文摘Oxidative coupling of α-bromoarylacetonitriles and oxidative decyanation of diarylacetonitriles are efficiently realized by solid-liquid phase transfer catalysis using anhydrous K 3 PO 4 as base and TBAB as catalyst in acetone at room temperature. In this mild and convenient method, α,β-dicyanostilbenes and diarylketones were prepared in good to excellent yields.
基金This work was financially supported by the National Nature Science Foundation of China(21272069,20672035)the Fundamental Reearch Funds for the Central Universities and Key Laboratory of Organofluorine Chemistry,Shanghai Institute of Organic Chemistry,Chinese Academy of Sciences.
文摘An efficient approach for the synthesis of N-arylated amides was developed via copper(Ⅱ) triflate-catalyzed direct oxidation of(aryl)methylamines to primary arylamides by air and subsequent N-arylation by diaryliodonium salts. Various substituted benzylamines could be applied in the reaction, providing a series of N-arylated amides in moderate to good yields. This method showed convenient, practical, and environment friendly advantages.
基金supported by the National Natural Science Foundation of China(21702151,21774029,and 21871211)the Fundamental Research Funds for Central Universities(2042019kf0208)。
文摘Synthesis of organosilanes from alkenes is a very important topic owing to their wide applications.A Ni/Cu dual metal-catalyzed arylsilylation of terminal alkenes,featuring migratory selectivity,has been developed.A wide diversity of aliphatic silanes have been prepared from terminal alkenes,aryl halides and Suginome’s reagent.This protocol is highlighted by excellent regioselectivity,mild reaction conditions and good functional group tolerance.In addition to benzylic positions,carbon–carbon bonds can also be constructed at allylic positions.Preliminary mechanistic studies suggest that the copper cocatalyst promotes the transmetalation of Suginome’s reagent,and the addition of a Pyr Ox ligand inhibits the formation of side-products from the carbon-Heck pathway.Moreover,studies toward the nature of the Pyr Ox ligand revealed that the steric hindrance of the oxazoline moiety greatly affects the chain–walking process,but not the arylation step.
