A series of 2-arylamino-1,3,5-triazine derivatives(4a–4g),which were designed and synthesized via Sonogashira coupling reaction,were evaluated using two-electrode voltage clamp(TEVC)recordings of humanα7 nAChR expre...A series of 2-arylamino-1,3,5-triazine derivatives(4a–4g),which were designed and synthesized via Sonogashira coupling reaction,were evaluated using two-electrode voltage clamp(TEVC)recordings of humanα7 nAChR expressed in Xenopus ooctyes.Compound 4g as a positive allosteric modulator(PAM)showed better efficacy than lead compound 3(HZZ-A-11)with an EC50 value of 1.23±0.41μM.Further pharmacological evaluation of compound 4g might lead to the developmental potential for therapy of cognitive deficits commonly shared by neuropsychiatric disorders,such as schizophrenia and Alzheimer’s disease.展开更多
CuI/ethylene diamine/K2CO3/dioxane is shown to be a useful system for the cross coupling reactions of various aryl iodides and bromides with aryl and alkyl alkynes. Compared to the conventional Sonogashira reactions, ...CuI/ethylene diamine/K2CO3/dioxane is shown to be a useful system for the cross coupling reactions of various aryl iodides and bromides with aryl and alkyl alkynes. Compared to the conventional Sonogashira reactions, the new procedure is free of palladium and phosphines.展开更多
A novel series of calix[4]arene derivatives were synthesized via a Pd-catalyzed Sonogashira coupling reaction from para-substituted iodobenzene and 25,27-dipropargyl-calix[4]arene. Fluorescence studies found that nitr...A novel series of calix[4]arene derivatives were synthesized via a Pd-catalyzed Sonogashira coupling reaction from para-substituted iodobenzene and 25,27-dipropargyl-calix[4]arene. Fluorescence studies found that nitro-phenols clearly exhibited quenching effects on 2c. Moreover, we minimized the free energy of the complexes by theoretical calculations. As the result, the πr-π stacking interactions take place between the 4-nitrophenol and calix[4]arene, which may lead to the significant fluorescence quench.展开更多
An efficient palladium-catalyzed copper- and amine-free Sonogashira coupling reaction of aryl bromides and chlorides was studied using a sterically hindered monooxychlorophosphine as new ligand.The use of 2 mol%Pd(OA...An efficient palladium-catalyzed copper- and amine-free Sonogashira coupling reaction of aryl bromides and chlorides was studied using a sterically hindered monooxychlorophosphine as new ligand.The use of 2 mol%Pd(OAc)_2 in the presence of K_2CO_3 allows the coupling reaction to proceed at mild condition with good to excellent yields.展开更多
Dendronized hyperbranched polymer (DHP) is a new kind of polymer, which combines the advantages of dendrimers and hy- perbranched polymers. In this work, two dendronized hyperbranched polymers, DttPG0 and DHPG1, wer...Dendronized hyperbranched polymer (DHP) is a new kind of polymer, which combines the advantages of dendrimers and hy- perbranched polymers. In this work, two dendronized hyperbranched polymers, DttPG0 and DHPG1, were successfully pre- pared through the simple "A3+B2" type Sonogashira coupling reaction. The nonlinear optical (NLO) effects of DHPG0 and DItPG1, characterized by the d33 values, were 183 and 220 pm V-1 respectively, higher than those of their analogues of den- dronized polymers and dendrimers, thanks to the special topological structure. Also, the obtained polymers displayed excellent solubility, good processability, and high thermal stability.展开更多
A novel approach to the synthesis of 4-phenylethynylphthalic anhydride has been described.The target compound was synthesized by Pd/Cu catalyzed Sonogashira coupling reaction between phenylacetylene and 4-bromophthali...A novel approach to the synthesis of 4-phenylethynylphthalic anhydride has been described.The target compound was synthesized by Pd/Cu catalyzed Sonogashira coupling reaction between phenylacetylene and 4-bromophthalic acid which was for the first time employed as start material,followed by dehydration of 4-phenylethynylphthalic acid.Compared with traditional synthetic routes,this method provides several advantages such as readily available raw materials,convenient manipulation and high yield.The products were characterized by IR,~1H NMR,^(13)C NMR,MS and elemental analysis,respectively.展开更多
基金National Natural Science Foundation of China aw arded to Q.Sun(NSFC,Grant No.81973169,21572011)and K.W.Wang(NSFC,Grant No.81537410)the Ministry of Science and Technology of China to K.W.Wang(Grant No.2014ZX09507003-006-004)。
文摘A series of 2-arylamino-1,3,5-triazine derivatives(4a–4g),which were designed and synthesized via Sonogashira coupling reaction,were evaluated using two-electrode voltage clamp(TEVC)recordings of humanα7 nAChR expressed in Xenopus ooctyes.Compound 4g as a positive allosteric modulator(PAM)showed better efficacy than lead compound 3(HZZ-A-11)with an EC50 value of 1.23±0.41μM.Further pharmacological evaluation of compound 4g might lead to the developmental potential for therapy of cognitive deficits commonly shared by neuropsychiatric disorders,such as schizophrenia and Alzheimer’s disease.
文摘CuI/ethylene diamine/K2CO3/dioxane is shown to be a useful system for the cross coupling reactions of various aryl iodides and bromides with aryl and alkyl alkynes. Compared to the conventional Sonogashira reactions, the new procedure is free of palladium and phosphines.
基金financially supported by the National Natural Science Foundation of China(Nos.21372092,21072072, 21102051)PCSIRT(No.IRT0953)+2 种基金Program for New Century Excellent Talent in University(No.NCET-10-0428)self-determined research funds of CCNU from the colleges,basic research and operation of MOE(Nos.CCNU11C01002,CCNU13F005)State Key Laboratory of Chemo/Biosensing and Chemometrics (201003)
文摘A novel series of calix[4]arene derivatives were synthesized via a Pd-catalyzed Sonogashira coupling reaction from para-substituted iodobenzene and 25,27-dipropargyl-calix[4]arene. Fluorescence studies found that nitro-phenols clearly exhibited quenching effects on 2c. Moreover, we minimized the free energy of the complexes by theoretical calculations. As the result, the πr-π stacking interactions take place between the 4-nitrophenol and calix[4]arene, which may lead to the significant fluorescence quench.
基金Henan University of Technology for financial support(The Introduction of Talent Fund)
文摘An efficient palladium-catalyzed copper- and amine-free Sonogashira coupling reaction of aryl bromides and chlorides was studied using a sterically hindered monooxychlorophosphine as new ligand.The use of 2 mol%Pd(OAc)_2 in the presence of K_2CO_3 allows the coupling reaction to proceed at mild condition with good to excellent yields.
基金supported by the National Natural Science Foundation of China(21325416)
文摘Dendronized hyperbranched polymer (DHP) is a new kind of polymer, which combines the advantages of dendrimers and hy- perbranched polymers. In this work, two dendronized hyperbranched polymers, DttPG0 and DHPG1, were successfully pre- pared through the simple "A3+B2" type Sonogashira coupling reaction. The nonlinear optical (NLO) effects of DHPG0 and DItPG1, characterized by the d33 values, were 183 and 220 pm V-1 respectively, higher than those of their analogues of den- dronized polymers and dendrimers, thanks to the special topological structure. Also, the obtained polymers displayed excellent solubility, good processability, and high thermal stability.
基金the National Undergraduates' Innovative Experiment Project of China and the Undergraduates' Innovative Experiment Project of Sichuan University for financial support
文摘A novel approach to the synthesis of 4-phenylethynylphthalic anhydride has been described.The target compound was synthesized by Pd/Cu catalyzed Sonogashira coupling reaction between phenylacetylene and 4-bromophthalic acid which was for the first time employed as start material,followed by dehydration of 4-phenylethynylphthalic acid.Compared with traditional synthetic routes,this method provides several advantages such as readily available raw materials,convenient manipulation and high yield.The products were characterized by IR,~1H NMR,^(13)C NMR,MS and elemental analysis,respectively.