In order to accelerate the development of relatively inexpensive antimalarials that are effective against chloroquine-resistant strains of Plasmodium falciparum, a methodology for the solid phase synthesis of chalcone...In order to accelerate the development of relatively inexpensive antimalarials that are effective against chloroquine-resistant strains of Plasmodium falciparum, a methodology for the solid phase synthesis of chalcone (1, 3-diphenyl-2-propen-1-one) analogues in reasonably high yields has been developed.展开更多
The solid-phase synthesis of isoxazolines on 2-polystyrylsulfonamidoethanol resin is reported. 2-Polystyrylsulfonamidoethanol resin 1 was reacted with acryloyl chloride to afford 2-polystyrylsulfonylamidoethyl acrylat...The solid-phase synthesis of isoxazolines on 2-polystyrylsulfonamidoethanol resin is reported. 2-Polystyrylsulfonamidoethanol resin 1 was reacted with acryloyl chloride to afford 2-polystyrylsulfonylamidoethyl acrylate resin 2, which was further reacted with brominated aldoximes by [3+2] cycloaddition to give isoxazoline resin 4. Resin 4 was treated with aqueous 6 mol/L HCl solution to obtain isoxazolines in good yield and purity.展开更多
A general method for the solid phase synthesis of hydro-uracils and thiouracils is described. Resino ester 2 reacts with various primary amines to give secondary amines 3, which are converted to the resino ureas (thio...A general method for the solid phase synthesis of hydro-uracils and thiouracils is described. Resino ester 2 reacts with various primary amines to give secondary amines 3, which are converted to the resino ureas (thioureas) 4 by treatment with isocyanates (isothiocyanates). Preparation of the hydro-uracils and thiouracils 5 is achieved by acidic cyclization-cleavage from the resin. The synthesis is designed to be amenable for structure based library approach to photosystem II D1 protein inhibitors.展开更多
Most of carbon dots(CDs) are synthesized in solutions, but the extensive use of solvents produces too much waste, needs complex purification and results in low yield. Particularly for the popular hydrothermal/solvothe...Most of carbon dots(CDs) are synthesized in solutions, but the extensive use of solvents produces too much waste, needs complex purification and results in low yield. Particularly for the popular hydrothermal/solvothermal syntheses, safety issues hinder the large-scale production of CDs. Solid phase synthesis in air seems perfect to solve the above problems once for all, but nanoparticle growth in solid phase is always difficult to control. Here we suggest a new method to synthesize CDs in SBA-15 template, just by heating single carbon sources in air. Employing single carbon sources is important, which ensures both homogeneity of the nucleation and uniformity of the nanoparticle growth. The pores confinement of SBA-15 guarantees the uniform sizes of CDs, while the catalytic effect of SBA-15 accelerates the carbonization process of precursors. The products are easily extracted from the template by ethanol, and then the template can be recycled for the next synthesis after calcination. Various CDs are synthesized in this way by using different carbon sources and SBA-15 templates with different pore diameters, respectively. The results show that, the fluorescence properties of these CDs are determined by their composition and surface states, but not the particle sizes. This work opens a new avenue to synthesize uniform CDs in solid phase with high yield, low cost and tunable luminescence.展开更多
Carboxycoumsrins were synthesized via the solid phase synthesis conviently. The resin bound cyclic malonic ester reacted with o-methoxy or o-hydroxybenzaldehydes. Then cyclization was processed under H2SO4 to afford...Carboxycoumsrins were synthesized via the solid phase synthesis conviently. The resin bound cyclic malonic ester reacted with o-methoxy or o-hydroxybenzaldehydes. Then cyclization was processed under H2SO4 to afford the products in excellent purities and yields.展开更多
A facile solid phase synthesis of ethyl β -substituted indolepropionates is reported. Condensation between indole,polymer-supported cyclic malonic acid ester and aldehyde yielded the trimolecular adducts,which was cl...A facile solid phase synthesis of ethyl β -substituted indolepropionates is reported. Condensation between indole,polymer-supported cyclic malonic acid ester and aldehyde yielded the trimolecular adducts,which was cleaved by pyridine/EtOH to release the final products in good yield with high purity.展开更多
A facile solid phase synthesis of 2-substituted 1,3-oxazin-6-ones using polymer-supported Meldrums acid has been reported. Reaction of the resin-bound cyclic malonic acid ester with triethyl orthoformate and subsequen...A facile solid phase synthesis of 2-substituted 1,3-oxazin-6-ones using polymer-supported Meldrums acid has been reported. Reaction of the resin-bound cyclic malonic acid ester with triethyl orthoformate and subsequent dou-ble substitution with amide, afforded the corresponding polymer-supported acylaminomethylene cyclic malonic acid ester, which upon thermal treatment led to 1, 3-oxazin-6-ones in good yields and with high purity.展开更多
A use of Sulfonate ester as a linker in synthesis of (-aminoalkanols was reported. Diols were tethered onto polystyryl sulfonyl chloride resin, yielding sulfonate resins (2). After cleaved by diethyl amine, diisopropy...A use of Sulfonate ester as a linker in synthesis of (-aminoalkanols was reported. Diols were tethered onto polystyryl sulfonyl chloride resin, yielding sulfonate resins (2). After cleaved by diethyl amine, diisopropylamine and propylamine respectively, three (-aminoalkanols were obtained.展开更多
Polystyrene-supported 4-(phenylseleno)morpholine was synthesized and could be used as an efficient ?selenenylating agent for saturated aldehydes. ?Haloaldehydes were prepared by reaction of polystyrene-supported ?sel...Polystyrene-supported 4-(phenylseleno)morpholine was synthesized and could be used as an efficient ?selenenylating agent for saturated aldehydes. ?Haloaldehydes were prepared by reaction of polystyrene-supported ?selenoaldehydes with bromine or sulfuryl chloride in good yield and high purity.展开更多
Reaction of polymer-supported a-selenoaldehydes with Grignard reagents afforded polymer-bound B-hydroxyalkyl selenides, which treated with thionyl chloride and triethylamine leading to (E)-1, 2-disubstituted ethenes i...Reaction of polymer-supported a-selenoaldehydes with Grignard reagents afforded polymer-bound B-hydroxyalkyl selenides, which treated with thionyl chloride and triethylamine leading to (E)-1, 2-disubstituted ethenes in good yield.展开更多
A 36-residue peptide is designed to cure acquired immunodeficiency syndrome(AIDS), and is synthesized by the manual solid phase peptide synthesis technique. Different reaction conditions of the synthesis process were ...A 36-residue peptide is designed to cure acquired immunodeficiency syndrome(AIDS), and is synthesized by the manual solid phase peptide synthesis technique. Different reaction conditions of the synthesis process were discussed. Stirring efficiency of mechanics and nitrogen was compared. The mechanical method displays a predominant performance. Although the coupling efficiencies of diisopropylcarbodiimide(DIC) and dicyclohexylcarbodiimide(DCC) are virtually identical, DIC offers several advantages over DCC in practice due to different physical characters. Wash conditions after deprotection and coupling were investigated to monitor washing efficiency. 0.369 2 g crude peptide was obtained.展开更多
A novel facile procedure for traceless solid-phase synthesis of 3-substituted isoxazoles in good yields and with excellent purities using polymer-supported vinyl selenide has been developed.
Reaction of polystyrene-supported lithium selenide with 3-acetoxy-2-methylene-alkanoates afforded the corresponding allyl selenide resins and subsequent cleavage from the polymer by treating with methyl iodide to furn...Reaction of polystyrene-supported lithium selenide with 3-acetoxy-2-methylene-alkanoates afforded the corresponding allyl selenide resins and subsequent cleavage from the polymer by treating with methyl iodide to furnish (Z)-allyl iodides in good yields and high purities. The polymeric selenium reagent can be regenerated and reused. So it is a environmentally benign reagent.展开更多
Sol sol gel method and solid phase redox reaction were respectively applied in preparation of Nanosize MnO 2 powders. The experiments showed that only Mn 2O 3 could be obtained from ignition of Mn(Ⅱ) in the muffle fu...Sol sol gel method and solid phase redox reaction were respectively applied in preparation of Nanosize MnO 2 powders. The experiments showed that only Mn 2O 3 could be obtained from ignition of Mn(Ⅱ) in the muffle furnace in air, and Mn 2O 3 had to be disproportionated in acids to gain MnO 2. The analysis of XRD and TEM technique revealed that the diameters of nanosize MnO 2 obtained by sol gel method was 35~45 nm and the x in MnO x was 1 9; the particle size of MnO 2 produced from solid phase redox reaction was 10~20 nm and the x in MnO x equaled 1 94. The test results have proved that the discharge property of alkaline manganese battery could be improved by nanosize MnO 2.展开更多
The synthesis of peptoid nucleic acid bearing thymine as nucleobase has been achieved. This modified oligonucleotide showed good hybridization with DNA.
基金grants from the Advanced Research Projects Agency (MDA-972-9l-J1013, N000l4-90-2032) and the World Health Organization (WHO 940l
文摘In order to accelerate the development of relatively inexpensive antimalarials that are effective against chloroquine-resistant strains of Plasmodium falciparum, a methodology for the solid phase synthesis of chalcone (1, 3-diphenyl-2-propen-1-one) analogues in reasonably high yields has been developed.
基金NNSFC (20074017,29844001) and Visiting Scholar Foundation of Key Lab. In University
文摘The solid-phase synthesis of isoxazolines on 2-polystyrylsulfonamidoethanol resin is reported. 2-Polystyrylsulfonamidoethanol resin 1 was reacted with acryloyl chloride to afford 2-polystyrylsulfonylamidoethyl acrylate resin 2, which was further reacted with brominated aldoximes by [3+2] cycloaddition to give isoxazoline resin 4. Resin 4 was treated with aqueous 6 mol/L HCl solution to obtain isoxazolines in good yield and purity.
文摘A general method for the solid phase synthesis of hydro-uracils and thiouracils is described. Resino ester 2 reacts with various primary amines to give secondary amines 3, which are converted to the resino ureas (thioureas) 4 by treatment with isocyanates (isothiocyanates). Preparation of the hydro-uracils and thiouracils 5 is achieved by acidic cyclization-cleavage from the resin. The synthesis is designed to be amenable for structure based library approach to photosystem II D1 protein inhibitors.
基金financially supported by the National Natural Science Foundation of China (Nos. 21975048, 21771039)the Shanghai Science and Technology Committee (No. 19DZ2270100)。
文摘Most of carbon dots(CDs) are synthesized in solutions, but the extensive use of solvents produces too much waste, needs complex purification and results in low yield. Particularly for the popular hydrothermal/solvothermal syntheses, safety issues hinder the large-scale production of CDs. Solid phase synthesis in air seems perfect to solve the above problems once for all, but nanoparticle growth in solid phase is always difficult to control. Here we suggest a new method to synthesize CDs in SBA-15 template, just by heating single carbon sources in air. Employing single carbon sources is important, which ensures both homogeneity of the nucleation and uniformity of the nanoparticle growth. The pores confinement of SBA-15 guarantees the uniform sizes of CDs, while the catalytic effect of SBA-15 accelerates the carbonization process of precursors. The products are easily extracted from the template by ethanol, and then the template can be recycled for the next synthesis after calcination. Various CDs are synthesized in this way by using different carbon sources and SBA-15 templates with different pore diameters, respectively. The results show that, the fluorescence properties of these CDs are determined by their composition and surface states, but not the particle sizes. This work opens a new avenue to synthesize uniform CDs in solid phase with high yield, low cost and tunable luminescence.
基金Project.20072032 was supported by the National Natural Science Foundation of China.
文摘Carboxycoumsrins were synthesized via the solid phase synthesis conviently. The resin bound cyclic malonic ester reacted with o-methoxy or o-hydroxybenzaldehydes. Then cyclization was processed under H2SO4 to afford the products in excellent purities and yields.
基金ProjectsupportedbytheNationalNaturalScienceFoundationofChina (No .2 0 0 72 0 3 2 )
文摘A facile solid phase synthesis of ethyl β -substituted indolepropionates is reported. Condensation between indole,polymer-supported cyclic malonic acid ester and aldehyde yielded the trimolecular adducts,which was cleaved by pyridine/EtOH to release the final products in good yield with high purity.
基金Project supported by the National Natural Science Foundation of China (No. 20072032).
文摘A facile solid phase synthesis of 2-substituted 1,3-oxazin-6-ones using polymer-supported Meldrums acid has been reported. Reaction of the resin-bound cyclic malonic acid ester with triethyl orthoformate and subsequent dou-ble substitution with amide, afforded the corresponding polymer-supported acylaminomethylene cyclic malonic acid ester, which upon thermal treatment led to 1, 3-oxazin-6-ones in good yields and with high purity.
基金NNSFC (20074017, 29844001) and Visiting Scholar Foundation of Key Lab. in University.
文摘A use of Sulfonate ester as a linker in synthesis of (-aminoalkanols was reported. Diols were tethered onto polystyryl sulfonyl chloride resin, yielding sulfonate resins (2). After cleaved by diethyl amine, diisopropylamine and propylamine respectively, three (-aminoalkanols were obtained.
文摘Polystyrene-supported 4-(phenylseleno)morpholine was synthesized and could be used as an efficient ?selenenylating agent for saturated aldehydes. ?Haloaldehydes were prepared by reaction of polystyrene-supported ?selenoaldehydes with bromine or sulfuryl chloride in good yield and high purity.
基金Project 29932020 was supported by the National Natural Science Foundation of China.
文摘Reaction of polymer-supported a-selenoaldehydes with Grignard reagents afforded polymer-bound B-hydroxyalkyl selenides, which treated with thionyl chloride and triethylamine leading to (E)-1, 2-disubstituted ethenes in good yield.
文摘A 36-residue peptide is designed to cure acquired immunodeficiency syndrome(AIDS), and is synthesized by the manual solid phase peptide synthesis technique. Different reaction conditions of the synthesis process were discussed. Stirring efficiency of mechanics and nitrogen was compared. The mechanical method displays a predominant performance. Although the coupling efficiencies of diisopropylcarbodiimide(DIC) and dicyclohexylcarbodiimide(DCC) are virtually identical, DIC offers several advantages over DCC in practice due to different physical characters. Wash conditions after deprotection and coupling were investigated to monitor washing efficiency. 0.369 2 g crude peptide was obtained.
基金We thank the National Natural Science Foundation of China(No.20562005)NSF of Jiangxi Province for financial support.
文摘A novel facile procedure for traceless solid-phase synthesis of 3-substituted isoxazoles in good yields and with excellent purities using polymer-supported vinyl selenide has been developed.
基金the National Natural Science Foundation of China (No. 20562005) NSF of Jiangxi Province (No. 0620021) for financial support.
文摘Reaction of polystyrene-supported lithium selenide with 3-acetoxy-2-methylene-alkanoates afforded the corresponding allyl selenide resins and subsequent cleavage from the polymer by treating with methyl iodide to furnish (Z)-allyl iodides in good yields and high purities. The polymeric selenium reagent can be regenerated and reused. So it is a environmentally benign reagent.
文摘Sol sol gel method and solid phase redox reaction were respectively applied in preparation of Nanosize MnO 2 powders. The experiments showed that only Mn 2O 3 could be obtained from ignition of Mn(Ⅱ) in the muffle furnace in air, and Mn 2O 3 had to be disproportionated in acids to gain MnO 2. The analysis of XRD and TEM technique revealed that the diameters of nanosize MnO 2 obtained by sol gel method was 35~45 nm and the x in MnO x was 1 9; the particle size of MnO 2 produced from solid phase redox reaction was 10~20 nm and the x in MnO x equaled 1 94. The test results have proved that the discharge property of alkaline manganese battery could be improved by nanosize MnO 2.
基金Authors thank the National NatUral Science Foundation of China for financial support !(29672047).
文摘The synthesis of peptoid nucleic acid bearing thymine as nucleobase has been achieved. This modified oligonucleotide showed good hybridization with DNA.