A series of new 2,5-disubstituted-l,3,4-oxadiazole and 1,2,4-triazole derivatives were synthesized by hetero- cyclization of acid hydrazide I and thiosemicarbazide derivative 2. Furthermore, the acyclic C-nucleoside a...A series of new 2,5-disubstituted-l,3,4-oxadiazole and 1,2,4-triazole derivatives were synthesized by hetero- cyclization of acid hydrazide I and thiosemicarbazide derivative 2. Furthermore, the acyclic C-nucleoside analogs were prepared by cyclization of their corresponding sugar hydrazones by reaction with acetic anhydride. The antimicrobial activity of the prepared compounds was evaluated and some of the synthesized compounds revealed good activities against fungi.展开更多
A simple metal and additive-free approach for the assembly of 5-trifluoromethyl-1,2,4-triazoles via only heatinginduced decarboxylative cyclization of readily available trifluoroacetimidohydrazides andα-oxocarboxylic...A simple metal and additive-free approach for the assembly of 5-trifluoromethyl-1,2,4-triazoles via only heatinginduced decarboxylative cyclization of readily available trifluoroacetimidohydrazides andα-oxocarboxylic acids has been developed.In this protocol,the rarely reported tetrahedral carboxylic acids intermediate could be in-situ generated and undergo subsequent decarboxylation to afford the target heterocycle products.展开更多
Agreen regioselective synthesis of some new and known 9-aryl-5,9-dihydropyrimido[4,5-d][l,2,4]triazolo[1,5-a]pyrimidine-6,8（4H,7H）-diones has been described via the microwave-assisted one-pot reaction of 3-amino-1H-...Agreen regioselective synthesis of some new and known 9-aryl-5,9-dihydropyrimido[4,5-d][l,2,4]triazolo[1,5-a]pyrimidine-6,8（4H,7H）-diones has been described via the microwave-assisted one-pot reaction of 3-amino-1H-1,2,4-triazoles,aromatic aldehydes and barbituric acids under solvent- and catalyst-free conditions.This operationally simple procedure is less laborious and provides a better scope than previously reported procedures.展开更多
Starting from the basic stock,ethyl phenylacetate and aryl amines,1benzylformy14ary1 thiosemicarbazides were prepared through multistep reactions.The ringclosure of 1benzylformy14ary1 thiosemicarbazides ...Starting from the basic stock,ethyl phenylacetate and aryl amines,1benzylformy14ary1 thiosemicarbazides were prepared through multistep reactions.The ringclosure of 1benzylformy14ary1 thiosemicarbazides at the presence of hydrazine hydrate afforded the title compounds,3benzy14amino5arylamino1,2,4triazoles,with structures confirmed by elemental analysis,IR,1H and13C NMR spectra.展开更多
New ribonucleoside analogues containing thio-substituted 1,3,4-triazole as heterocyclic base have been synthesized via condensation of the central intermediate 1 with various acids, esters, amides, and anhydrides in a...New ribonucleoside analogues containing thio-substituted 1,3,4-triazole as heterocyclic base have been synthesized via condensation of the central intermediate 1 with various acids, esters, amides, and anhydrides in anhydrous solvent followed by deprotection.展开更多
A dinuclear Cu(Ⅱ) complex [Cu2(MMBPT)2Cl4(H2O)2.5] (I) [MMBPT=3-Methyl-4-(4-Methylphenyl)-5-(2-pyridyl)-1,2,4-triazole] was synthesized by reaction of MMBPT with CuCl2.2H2O and its structure was determined by X-ray c...A dinuclear Cu(Ⅱ) complex [Cu2(MMBPT)2Cl4(H2O)2.5] (I) [MMBPT=3-Methyl-4-(4-Methylphenyl)-5-(2-pyridyl)-1,2,4-triazole] was synthesized by reaction of MMBPT with CuCl2.2H2O and its structure was determined by X-ray crystal structure analysis. The structure indicates that the complex crystallizes in monoclinic,space group P21/c with a=1.273 4(3) nm,b=1.237 5(3) nm,c=2.403 2(5) nm,β=90.51(3)°. V=3.786 6(13) nm3,Z=2,Dc=1.429 Mg.m-3,μ=1.445 mm-1,F(000)=1 660,and final R1=0.055 5,wR2=0.129 7. The crystal structure shows that the dinuclear Cu2N6 unit is almost planar in which each Cu(Ⅱ)ion was five-coordinated by one nitrogen atoms from MMBPT and two chlorine in the basal positions and two nitrogen atoms from two MMBPTs respectively in the axial one,to form a distorted trigonal bipyramidal geometry. Magnetic measurements reveal a relatively strong antiferromagentic interaction in the complex. CCDC:720011.展开更多
文摘A series of new 2,5-disubstituted-l,3,4-oxadiazole and 1,2,4-triazole derivatives were synthesized by hetero- cyclization of acid hydrazide I and thiosemicarbazide derivative 2. Furthermore, the acyclic C-nucleoside analogs were prepared by cyclization of their corresponding sugar hydrazones by reaction with acetic anhydride. The antimicrobial activity of the prepared compounds was evaluated and some of the synthesized compounds revealed good activities against fungi.
基金support from the Natural Science Foundation of Zhejiang Province(No.LY19B020016)the K.C.Wong Education Foundation(No.GJTD-2020-08).
文摘A simple metal and additive-free approach for the assembly of 5-trifluoromethyl-1,2,4-triazoles via only heatinginduced decarboxylative cyclization of readily available trifluoroacetimidohydrazides andα-oxocarboxylic acids has been developed.In this protocol,the rarely reported tetrahedral carboxylic acids intermediate could be in-situ generated and undergo subsequent decarboxylation to afford the target heterocycle products.
文摘Agreen regioselective synthesis of some new and known 9-aryl-5,9-dihydropyrimido[4,5-d][l,2,4]triazolo[1,5-a]pyrimidine-6,8（4H,7H）-diones has been described via the microwave-assisted one-pot reaction of 3-amino-1H-1,2,4-triazoles,aromatic aldehydes and barbituric acids under solvent- and catalyst-free conditions.This operationally simple procedure is less laborious and provides a better scope than previously reported procedures.
文摘Starting from the basic stock,ethyl phenylacetate and aryl amines,1benzylformy14ary1 thiosemicarbazides were prepared through multistep reactions.The ringclosure of 1benzylformy14ary1 thiosemicarbazides at the presence of hydrazine hydrate afforded the title compounds,3benzy14amino5arylamino1,2,4triazoles,with structures confirmed by elemental analysis,IR,1H and13C NMR spectra.
文摘New ribonucleoside analogues containing thio-substituted 1,3,4-triazole as heterocyclic base have been synthesized via condensation of the central intermediate 1 with various acids, esters, amides, and anhydrides in anhydrous solvent followed by deprotection.
文摘A dinuclear Cu(Ⅱ) complex [Cu2(MMBPT)2Cl4(H2O)2.5] (I) [MMBPT=3-Methyl-4-(4-Methylphenyl)-5-(2-pyridyl)-1,2,4-triazole] was synthesized by reaction of MMBPT with CuCl2.2H2O and its structure was determined by X-ray crystal structure analysis. The structure indicates that the complex crystallizes in monoclinic,space group P21/c with a=1.273 4(3) nm,b=1.237 5(3) nm,c=2.403 2(5) nm,β=90.51(3)°. V=3.786 6(13) nm3,Z=2,Dc=1.429 Mg.m-3,μ=1.445 mm-1,F(000)=1 660,and final R1=0.055 5,wR2=0.129 7. The crystal structure shows that the dinuclear Cu2N6 unit is almost planar in which each Cu(Ⅱ)ion was five-coordinated by one nitrogen atoms from MMBPT and two chlorine in the basal positions and two nitrogen atoms from two MMBPTs respectively in the axial one,to form a distorted trigonal bipyramidal geometry. Magnetic measurements reveal a relatively strong antiferromagentic interaction in the complex. CCDC:720011.
