Chiral carbonyl compounds frequently occur in natural products and pharmaceuticals. Additionally, they serve as important intermediates in organic synthesis. Transition metal-catalyzed asymmetric carbonylative cross-c...Chiral carbonyl compounds frequently occur in natural products and pharmaceuticals. Additionally, they serve as important intermediates in organic synthesis. Transition metal-catalyzed asymmetric carbonylative cross-coupling reactions are among the most straightforward and effective methods for synthesizing chiral carbonyl compounds, including esters, amides, and ketones. The advances in asymmetric carbonylative cross-coupling reactions using various O-, N-, C-, and S-containing nucleophiles or electrophiles over the past decade are summarized.展开更多
The Pd-catalyzed Suzuki-Miyaura coupling reaction is a crucial tool for constructing C-C bonds.Currently,the organic solvents employed during reaction may cause serious environmental problems.Moreover,the low solubili...The Pd-catalyzed Suzuki-Miyaura coupling reaction is a crucial tool for constructing C-C bonds.Currently,the organic solvents employed during reaction may cause serious environmental problems.Moreover,the low solubility of inorganic bases in organic solvents leads to enormous mass transfer resistance.To address this issue,the Pickering droplets reactor stabilized by Pd/g-C_(3)N_(4)at substrate-water two-phase interface is reported.Benefiting from the hydrophobic conjugated framework and hydrophilic terminal groups,Pd/g-C_(3)N_(4)can configure stable Pickering emulsion without additional functionalization.The Pd loaded catalysts exhibits excellent performance(TOF=21852 h^(-1))for the Suzuki-Miyaura coupling reaction,which is deriving from unique electronic structure of g-C_(3)N_(4)and high interfacial area of emulsion.Moreover,there is no clear decrease in reactivity after six cycles(conversion>86%).In this study,the organic solvent was replaced by reaction substrate,and the high activity can be achieved for various halogenated aromatic hydrocarbons and their derivatives.展开更多
A simple Cu（OAc）2 catalyzed Sonogashira coupling protocol is presented. It was found that the couplings of a variety of aryl halides with terminal alkynes were conducted smoothly to afford the corresponding desired ...A simple Cu（OAc）2 catalyzed Sonogashira coupling protocol is presented. It was found that the couplings of a variety of aryl halides with terminal alkynes were conducted smoothly to afford the corresponding desired products in moderate to excellent yields, using Cu（OAc）2 as the catalyst and Et3N as the solvent.展开更多
Surface-enhanced Raman spectroscopy(SERS), a powerful surface vibrational spectroscopic technique, is ideally suited for in situ monitoring the chemical transformations occurred at surfaces and/or interfaces.For in si...Surface-enhanced Raman spectroscopy(SERS), a powerful surface vibrational spectroscopic technique, is ideally suited for in situ monitoring the chemical transformations occurred at surfaces and/or interfaces.For in situ SERS monitoring, a platform integrated both plasmonic and catalytic activity is a prerequisite. Here, we fabricate a bifunctional Au-Pd nanocoronal film for in situ SERS monitoring Suzuki-Miyaura cross-coupling reaction. This excellent bifunctional substrate leads to the coupling of high catalytic activity with a strong SERS effect at the center of two adjacent Au cores and shows fine reproducibility and stability of SERS signals. During investigating the Suzuki reaction with in situ SERS, we found two distinct catalytic kinetic processes resulted from two disparate catalytic sites on a Au-Pd nanocoronal. Comparing with conventional analytical techniques, this work provides a novel approach for studying Suzuki reactions at surfaces and/or interfaces with in situ SERS.展开更多
Highly active, air-stable and water-soluble palladium-phosphinous acid complexes have been applied to Suzuki cross-coupling reaction of heteroaryl bromides under mild conditions in water/alcoholic solvents. Suzuki cro...Highly active, air-stable and water-soluble palladium-phosphinous acid complexes have been applied to Suzuki cross-coupling reaction of heteroaryl bromides under mild conditions in water/alcoholic solvents. Suzuki cross-coupling reaction of heteroaryl bromides with phenylboronic acid occurred efficiently using palladium phosphinous acid complexes （POPd） and phase transfer catalyst （tetrabutylammonium bromide and polyethylene glycol） in water/ethanol mixture, water/propanol mixture and neat water respectively, the corresponding yields of cross-coupling heteroaryl-aryls were satisfied. The tert-butyl substituted ligand di-tert-butylphosphino in combination with POPd was found to be more active than the same family derived catalysts dipalladium complexes POPdl and POPd2, and other two kinds of Pd-catalysts Pd（PPh3）4 and Pd2（dba）3. The mechanism of Suzuki cross-coupling reaction between heteroaryl bromides and phenylboronic acid in water was proposed with respect to the key role of phase transfer catalyst on the transmetallation step. Compared with other solid phase transfer catalysts, TBAB was tested as the ideal one. The alkalinity of base and the molar proportion between POPd and TBAB were investigated in water and alcoholic solvents. Notably, in the presence of TBAB adding alcoholic solvents into water enhanced the yields of target products. However in terms of the liquid phase transfer catalyst of PEGs, mixing water into PEGs could slightly decrease the yields with respect to the water free PEGs bulk phase, which was probably due to the homogenous liquid conditions in pure PEGs and weak interactions between PEGs and heteroaryl bromide molecules in water depending on their molecular chain lengths.展开更多
The present paper deals with the polymerization of ( R ) 3,3′ diiodo 2,2′ binaphtho 20 crown 6 with \{ p divinylbenzene\} under Heck coupling reaction condition. Both the monomers and the polymer were analyzed by NM...The present paper deals with the polymerization of ( R ) 3,3′ diiodo 2,2′ binaphtho 20 crown 6 with \{ p divinylbenzene\} under Heck coupling reaction condition. Both the monomers and the polymer were analyzed by NMR, FTIR, UV, CD, fluorescent spectroscopy, polarimetry, GPC and elemental analysis. The polymer can emit a strong blue fluorescence and is expected to have the potential application in the polarized blue light emitting sensors. The chiral conjugated polymer exhibits a strong Cotton effect in its Circular Dichroism(CD ) spectrum, indicating the high rigidity of the polymer backbone.展开更多
Pyrazoles and their derivatives are important heterocycles found in nature and present in numerous bioactive compounds.In contrast to 3 or 5-aryl pyrazole,the preparation of 4-aryl pyrazole is fairly rare.Utilizing mi...Pyrazoles and their derivatives are important heterocycles found in nature and present in numerous bioactive compounds.In contrast to 3 or 5-aryl pyrazole,the preparation of 4-aryl pyrazole is fairly rare.Utilizing microwave irradiation,the synthesis of 4-substituted-arylpyrazole via Suzuki cross-coupling has been developed with a wide range of substrates.The remarkable advantages of this method are mild reaction conditions,simple operation,high yield,and short reaction time.Product structures were identified by MS 1H NMR 13C NMR,and elemental analysis.展开更多
The preparation of Pd-based catalysts with rich electrons and a high atom dispersion rate is of great significance for improving the reactivity of cross-coupling reactions,which is a powerful tool for pharmaceutical a...The preparation of Pd-based catalysts with rich electrons and a high atom dispersion rate is of great significance for improving the reactivity of cross-coupling reactions,which is a powerful tool for pharmaceutical and fine chemical synthesis.Here,we report a PdNi single-atom alloy(SAA)catalyst in which isolated Pd single atoms are anchored onto the surface of Ni nanoparticles(NPs)applied for Suzuki coupling reactions and Heck coupling reactions.The 0.1%PdNi SAA exhibits extraordinary catalytic activity(reaction rate:17,032.25 mmol h^(-1)gPd^(-1))toward the Suzuki cross-coupling reaction between 4-bromoanisole and phenylboronic acid at 80℃for 1 h.The excellent activity is supposed to attribute to the 100 percent utilization rate of Pd atoms and the highly stable surface zero-valance Pd atoms,which provides abundant sites and electrons for the adsorption and fracture of the C-X(X=Cl,Br,I)bond.Moreover,our work demonstrates the excellent application prospect of SAAs for cross-coupling reactions.展开更多
In order to improve the yield and reduce the cost in the synthesis of antitumor drug vismodegib the key intermediates are prepared and the Negishi reaction step is examined.The effects of different molar ratios of rea...In order to improve the yield and reduce the cost in the synthesis of antitumor drug vismodegib the key intermediates are prepared and the Negishi reaction step is examined.The effects of different molar ratios of reactants dosages of catalyst and time for refluxing are investigated by using single factor tests.The results demonstrate that when the molar ratios of 2-bromopyridine 2-chloro-N-4-chloro-3-iodophenyl -4-methylsulfonyl benzamide zinc chloride n-butyllithium and tetrakis triphenyl phosphine palladium are changed to 1.0∶0.5∶1.5∶1.1∶0.05 and the mixture is refluxed for 24 h the production yield is improved to 72%.This reaction condition significantly enhances the synthetic efficiency avoids consuming excessive raw materials/catalysts and meanwhile prevents a prolonged reaction time.The optimization of the proportion of reactants and the heating time is proved to be important for the efficiency and economy in cross-coupling reaction to synthesize vismodegib.展开更多
Treatment of acyl chlorides and diaryl ketones with an activated Ti(o)reagent,prepared by reduction of TiCl_4 with Zn powder,effects an intermolecular reductive cross-coupling reaction leading to ketones.
Palladium-catalyzed cross-coupling reaction between dichlorotriazines and phenylboronate esters produced the mono-awlated triazines selectively and thus, the corresponding phenyltriazine derivatives could be assembled...Palladium-catalyzed cross-coupling reaction between dichlorotriazines and phenylboronate esters produced the mono-awlated triazines selectively and thus, the corresponding phenyltriazine derivatives could be assembled efficiently in moderate to good overall yields （50-80%）.展开更多
The system,Pd（OAc）_2/imidazolium salts（L_2）,was found as an efficient catalyst in the Heck coupling reaction of olefins with aryl halides and Suzuki reactions of various aryl halides with aryl boronic acids under ...The system,Pd（OAc）_2/imidazolium salts（L_2）,was found as an efficient catalyst in the Heck coupling reaction of olefins with aryl halides and Suzuki reactions of various aryl halides with aryl boronic acids under aerobic condition.This catalytic system demonstrates great tolerance to a wide range of groups on all substrates of aryl halides,alkenes and aryl boronic acids.展开更多
Polymer-supported phosphine ligand 3b derived from ferrocene was prepared, and applied in palladium-catalyzed Suzuki- Miyaura reactions. A range of aryl bromides can couple with phenylboronic acid to obtain correspond...Polymer-supported phosphine ligand 3b derived from ferrocene was prepared, and applied in palladium-catalyzed Suzuki- Miyaura reactions. A range of aryl bromides can couple with phenylboronic acid to obtain corresponding biaryls in excellent yields. The recycling of the polymer-bound catalyst was tested without adding palladium.展开更多
Four aryl-guanidines（AG） were synthesized and used for the palladium-catalyzed Suzuki cross-coupling reaction to test the catalytic activity.In the presence of steric bulk AG,when aryl bromide and arylboronic acid w...Four aryl-guanidines（AG） were synthesized and used for the palladium-catalyzed Suzuki cross-coupling reaction to test the catalytic activity.In the presence of steric bulk AG,when aryl bromide and arylboronic acid were used as the reactants,the Suzuki reaction could be carried out smoothly at room temperature in aqueous solvent to afford the cross-coupling product in high yield.This catalysis system was also successful for the coupling of activated aryl chlorides at room temperature.展开更多
We describe a convenient method for the synthesis of 1,2-disubstituted acetylenes via a cross-coupling reaction of （bromoethynyl）benzene with Grignard reagents. The reaction of （bromoethynyl）benzene （1 mmol） wit...We describe a convenient method for the synthesis of 1,2-disubstituted acetylenes via a cross-coupling reaction of （bromoethynyl）benzene with Grignard reagents. The reaction of （bromoethynyl）benzene （1 mmol） with Grignard reagent （1.3 mmol） mediated by NiCl2 （4 mol%） and （p-CH3Ph）3P （8 mol%） in THF could produce 1,2-disubstituted acetylenes in good yields at room temperature.展开更多
A novel 4-anilinoquinazoline dimer linked by a carbon-carbon bond in the C-7 position was synthesized via a one step Suzuki cross-coupling reaction. All structures of new compounds were characterized by ^1H NMR, ^13C ...A novel 4-anilinoquinazoline dimer linked by a carbon-carbon bond in the C-7 position was synthesized via a one step Suzuki cross-coupling reaction. All structures of new compounds were characterized by ^1H NMR, ^13C NMR, and HRMS. The inhibition rate of the synthetic 4-anilinoquinazoline dimer 8 against epidermal growth factor receptor-tyrosine kinase enzymes （EGFR） in vitro was 44.4% at the concentration of 5.5 μmol/L.展开更多
The commercially available diphosphane ligand MeO-BIPHEP was first investigated in the palladium-catalyzed Sonogashira reaction in the absence of copper and amine.The coupling of various aryl bromides and aryl chlorid...The commercially available diphosphane ligand MeO-BIPHEP was first investigated in the palladium-catalyzed Sonogashira reaction in the absence of copper and amine.The coupling of various aryl bromides and aryl chlorides with phenylacetylene gave moderate to excellent yields.展开更多
The phosphazane derivatives （L1-3） were readily obtained by reaction of different ratios of PCI3 and PhNH2. The L1_3 derivatives were found to be efficient ligands in the palladium-catalyzed Suzuki C-C coupling reac...The phosphazane derivatives （L1-3） were readily obtained by reaction of different ratios of PCI3 and PhNH2. The L1_3 derivatives were found to be efficient ligands in the palladium-catalyzed Suzuki C-C coupling reactions in water. It was determined that with the use of L1-3/Pd（OAc）2 system as a catalyst, aryl halides undergo Suzuki cross-couplings with arylboronic acids to give the desired products in moderate to excellent yields.展开更多
文摘Chiral carbonyl compounds frequently occur in natural products and pharmaceuticals. Additionally, they serve as important intermediates in organic synthesis. Transition metal-catalyzed asymmetric carbonylative cross-coupling reactions are among the most straightforward and effective methods for synthesizing chiral carbonyl compounds, including esters, amides, and ketones. The advances in asymmetric carbonylative cross-coupling reactions using various O-, N-, C-, and S-containing nucleophiles or electrophiles over the past decade are summarized.
基金the National Natural Science Foundation of China(22178243).
文摘The Pd-catalyzed Suzuki-Miyaura coupling reaction is a crucial tool for constructing C-C bonds.Currently,the organic solvents employed during reaction may cause serious environmental problems.Moreover,the low solubility of inorganic bases in organic solvents leads to enormous mass transfer resistance.To address this issue,the Pickering droplets reactor stabilized by Pd/g-C_(3)N_(4)at substrate-water two-phase interface is reported.Benefiting from the hydrophobic conjugated framework and hydrophilic terminal groups,Pd/g-C_(3)N_(4)can configure stable Pickering emulsion without additional functionalization.The Pd loaded catalysts exhibits excellent performance(TOF=21852 h^(-1))for the Suzuki-Miyaura coupling reaction,which is deriving from unique electronic structure of g-C_(3)N_(4)and high interfacial area of emulsion.Moreover,there is no clear decrease in reactivity after six cycles(conversion>86%).In this study,the organic solvent was replaced by reaction substrate,and the high activity can be achieved for various halogenated aromatic hydrocarbons and their derivatives.
文摘A simple Cu（OAc）2 catalyzed Sonogashira coupling protocol is presented. It was found that the couplings of a variety of aryl halides with terminal alkynes were conducted smoothly to afford the corresponding desired products in moderate to excellent yields, using Cu（OAc）2 as the catalyst and Et3N as the solvent.
基金the financial support from the National Natural Science Foundation of China (No. 22022406)the Natural Science Foundation of Tianjin (Nos. 20JCJQJC00110 and 20JCYBJC00590)+1 种基金the 111 project (No. B12015)the Haihe Laboratory of Sustainable Chemical Transformations。
文摘Surface-enhanced Raman spectroscopy(SERS), a powerful surface vibrational spectroscopic technique, is ideally suited for in situ monitoring the chemical transformations occurred at surfaces and/or interfaces.For in situ SERS monitoring, a platform integrated both plasmonic and catalytic activity is a prerequisite. Here, we fabricate a bifunctional Au-Pd nanocoronal film for in situ SERS monitoring Suzuki-Miyaura cross-coupling reaction. This excellent bifunctional substrate leads to the coupling of high catalytic activity with a strong SERS effect at the center of two adjacent Au cores and shows fine reproducibility and stability of SERS signals. During investigating the Suzuki reaction with in situ SERS, we found two distinct catalytic kinetic processes resulted from two disparate catalytic sites on a Au-Pd nanocoronal. Comparing with conventional analytical techniques, this work provides a novel approach for studying Suzuki reactions at surfaces and/or interfaces with in situ SERS.
基金supported by the Natural Science Foundation of Liaoning Education Department (No. 2008T094)
文摘Highly active, air-stable and water-soluble palladium-phosphinous acid complexes have been applied to Suzuki cross-coupling reaction of heteroaryl bromides under mild conditions in water/alcoholic solvents. Suzuki cross-coupling reaction of heteroaryl bromides with phenylboronic acid occurred efficiently using palladium phosphinous acid complexes （POPd） and phase transfer catalyst （tetrabutylammonium bromide and polyethylene glycol） in water/ethanol mixture, water/propanol mixture and neat water respectively, the corresponding yields of cross-coupling heteroaryl-aryls were satisfied. The tert-butyl substituted ligand di-tert-butylphosphino in combination with POPd was found to be more active than the same family derived catalysts dipalladium complexes POPdl and POPd2, and other two kinds of Pd-catalysts Pd（PPh3）4 and Pd2（dba）3. The mechanism of Suzuki cross-coupling reaction between heteroaryl bromides and phenylboronic acid in water was proposed with respect to the key role of phase transfer catalyst on the transmetallation step. Compared with other solid phase transfer catalysts, TBAB was tested as the ideal one. The alkalinity of base and the molar proportion between POPd and TBAB were investigated in water and alcoholic solvents. Notably, in the presence of TBAB adding alcoholic solvents into water enhanced the yields of target products. However in terms of the liquid phase transfer catalyst of PEGs, mixing water into PEGs could slightly decrease the yields with respect to the water free PEGs bulk phase, which was probably due to the homogenous liquid conditions in pure PEGs and weak interactions between PEGs and heteroaryl bromide molecules in water depending on their molecular chain lengths.
文摘The present paper deals with the polymerization of ( R ) 3,3′ diiodo 2,2′ binaphtho 20 crown 6 with \{ p divinylbenzene\} under Heck coupling reaction condition. Both the monomers and the polymer were analyzed by NMR, FTIR, UV, CD, fluorescent spectroscopy, polarimetry, GPC and elemental analysis. The polymer can emit a strong blue fluorescence and is expected to have the potential application in the polarized blue light emitting sensors. The chiral conjugated polymer exhibits a strong Cotton effect in its Circular Dichroism(CD ) spectrum, indicating the high rigidity of the polymer backbone.
基金the National Nature Science Foundation of China (Nos. 21002038 and 21272091) for the financial support
文摘Pyrazoles and their derivatives are important heterocycles found in nature and present in numerous bioactive compounds.In contrast to 3 or 5-aryl pyrazole,the preparation of 4-aryl pyrazole is fairly rare.Utilizing microwave irradiation,the synthesis of 4-substituted-arylpyrazole via Suzuki cross-coupling has been developed with a wide range of substrates.The remarkable advantages of this method are mild reaction conditions,simple operation,high yield,and short reaction time.Product structures were identified by MS 1H NMR 13C NMR,and elemental analysis.
基金supported by the financial aid from National Science and Technology Major Project of China(No.2021YFB3500700)National Natural Science Foundation of China(Nos.22020102003,22025506 and 22271274)Program of Science and Technology Development Plan of Jilin Province of China(Nos.20230101035JC and 20230101022JC)。
文摘The preparation of Pd-based catalysts with rich electrons and a high atom dispersion rate is of great significance for improving the reactivity of cross-coupling reactions,which is a powerful tool for pharmaceutical and fine chemical synthesis.Here,we report a PdNi single-atom alloy(SAA)catalyst in which isolated Pd single atoms are anchored onto the surface of Ni nanoparticles(NPs)applied for Suzuki coupling reactions and Heck coupling reactions.The 0.1%PdNi SAA exhibits extraordinary catalytic activity(reaction rate:17,032.25 mmol h^(-1)gPd^(-1))toward the Suzuki cross-coupling reaction between 4-bromoanisole and phenylboronic acid at 80℃for 1 h.The excellent activity is supposed to attribute to the 100 percent utilization rate of Pd atoms and the highly stable surface zero-valance Pd atoms,which provides abundant sites and electrons for the adsorption and fracture of the C-X(X=Cl,Br,I)bond.Moreover,our work demonstrates the excellent application prospect of SAAs for cross-coupling reactions.
基金The National Basic Research Program of China(973Program)(No.2011CB933503)China Postdoctoral Science Foundation(No.2013M541592)
文摘In order to improve the yield and reduce the cost in the synthesis of antitumor drug vismodegib the key intermediates are prepared and the Negishi reaction step is examined.The effects of different molar ratios of reactants dosages of catalyst and time for refluxing are investigated by using single factor tests.The results demonstrate that when the molar ratios of 2-bromopyridine 2-chloro-N-4-chloro-3-iodophenyl -4-methylsulfonyl benzamide zinc chloride n-butyllithium and tetrakis triphenyl phosphine palladium are changed to 1.0∶0.5∶1.5∶1.1∶0.05 and the mixture is refluxed for 24 h the production yield is improved to 72%.This reaction condition significantly enhances the synthetic efficiency avoids consuming excessive raw materials/catalysts and meanwhile prevents a prolonged reaction time.The optimization of the proportion of reactants and the heating time is proved to be important for the efficiency and economy in cross-coupling reaction to synthesize vismodegib.
文摘Treatment of acyl chlorides and diaryl ketones with an activated Ti(o)reagent,prepared by reduction of TiCl_4 with Zn powder,effects an intermolecular reductive cross-coupling reaction leading to ketones.
基金the National Natural Science Foundation of China(Nos.30873137,30772645 and 81172927) for their financial support
文摘Palladium-catalyzed cross-coupling reaction between dichlorotriazines and phenylboronate esters produced the mono-awlated triazines selectively and thus, the corresponding phenyltriazine derivatives could be assembled efficiently in moderate to good overall yields （50-80%）.
基金the Research Council of University of Maragheh for financially support of this workM.B.thanks the Sharif University of Technology for funding of this work
文摘The system,Pd（OAc）_2/imidazolium salts（L_2）,was found as an efficient catalyst in the Heck coupling reaction of olefins with aryl halides and Suzuki reactions of various aryl halides with aryl boronic acids under aerobic condition.This catalytic system demonstrates great tolerance to a wide range of groups on all substrates of aryl halides,alkenes and aryl boronic acids.
基金This work was financially supported by the Knowledge Innovation Program of the Chinese Academy of Sciences(DICP R200309)the National Basic Research Program of China(2003CB61615803)the National Natural Science Foundation of China(No.20473089).
文摘Polymer-supported phosphine ligand 3b derived from ferrocene was prepared, and applied in palladium-catalyzed Suzuki- Miyaura reactions. A range of aryl bromides can couple with phenylboronic acid to obtain corresponding biaryls in excellent yields. The recycling of the polymer-bound catalyst was tested without adding palladium.
基金Supported by the National Natural Science Foundation of China(Nos.20802071,21074133)
文摘Four aryl-guanidines（AG） were synthesized and used for the palladium-catalyzed Suzuki cross-coupling reaction to test the catalytic activity.In the presence of steric bulk AG,when aryl bromide and arylboronic acid were used as the reactants,the Suzuki reaction could be carried out smoothly at room temperature in aqueous solvent to afford the cross-coupling product in high yield.This catalysis system was also successful for the coupling of activated aryl chlorides at room temperature.
基金financially supported by the Fundamental Research Funds for the Central Universities,Southwest University for Nationalities (No.12NZYTH03)the Natural Science Foundation of Southwest University for Nationalities (No.381010)+1 种基金the Project of Postgraduate Degree Construction,Southwest University for Nationalities (No.2013XWD-S0703)the State Administration of Foreign Experts Affairs project (No.2012-10)
文摘We describe a convenient method for the synthesis of 1,2-disubstituted acetylenes via a cross-coupling reaction of （bromoethynyl）benzene with Grignard reagents. The reaction of （bromoethynyl）benzene （1 mmol） with Grignard reagent （1.3 mmol） mediated by NiCl2 （4 mol%） and （p-CH3Ph）3P （8 mol%） in THF could produce 1,2-disubstituted acetylenes in good yields at room temperature.
基金the financial support of Key International S&T Cooperation Projects(No.2008DFA31040 and No.2009DFA32080) of Ministry of Science and Technology of the People's Republic of China
文摘A novel 4-anilinoquinazoline dimer linked by a carbon-carbon bond in the C-7 position was synthesized via a one step Suzuki cross-coupling reaction. All structures of new compounds were characterized by ^1H NMR, ^13C NMR, and HRMS. The inhibition rate of the synthetic 4-anilinoquinazoline dimer 8 against epidermal growth factor receptor-tyrosine kinase enzymes （EGFR） in vitro was 44.4% at the concentration of 5.5 μmol/L.
文摘The commercially available diphosphane ligand MeO-BIPHEP was first investigated in the palladium-catalyzed Sonogashira reaction in the absence of copper and amine.The coupling of various aryl bromides and aryl chlorides with phenylacetylene gave moderate to excellent yields.
基金the Research Council of University of Maragheh and Shahid Chamran University for funding of this work
文摘The phosphazane derivatives （L1-3） were readily obtained by reaction of different ratios of PCI3 and PhNH2. The L1_3 derivatives were found to be efficient ligands in the palladium-catalyzed Suzuki C-C coupling reactions in water. It was determined that with the use of L1-3/Pd（OAc）2 system as a catalyst, aryl halides undergo Suzuki cross-couplings with arylboronic acids to give the desired products in moderate to excellent yields.
