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2017 Volume 37 Issue 6
2017, 37(6): 1309-1321
doi: 10.6023/cjoc201701031
Abstract:
Carbon dioxide is a cheap, abundant and renewable C1 feedstock. Methodology study on the transformation of carbon dioxide into highly value-added chemicals has become one of the most active topics in organic chemistry. Owing to the diversity of cycli...
Carbon dioxide is a cheap, abundant and renewable C1 feedstock. Methodology study on the transformation of carbon dioxide into highly value-added chemicals has become one of the most active topics in organic chemistry. Owing to the diversity of cycli...
2017, 37(6): 1322-1337
doi: 10.6023/cjoc201702051
Abstract:
Palladium-catalyzed cross-coupling reactions have been developed for decades as useful methods in organic synthesis. Compared to aryl and alkenyl halides, alkyl halides are more challenging to be applied in cross-coupling reactions. This mainly arise...
Palladium-catalyzed cross-coupling reactions have been developed for decades as useful methods in organic synthesis. Compared to aryl and alkenyl halides, alkyl halides are more challenging to be applied in cross-coupling reactions. This mainly arise...
2017, 37(6): 1338-1351
doi: 10.6023/cjoc201702022
Abstract:
The ketones are important intermediates for the synthesis of fine chemicals, such as pharmaceuticals, natural products, agricultural chemicals, dyes, etc. The oxidation of C—H bonds is one of the most direct and efficient synthetic methods for the p...
The ketones are important intermediates for the synthesis of fine chemicals, such as pharmaceuticals, natural products, agricultural chemicals, dyes, etc. The oxidation of C—H bonds is one of the most direct and efficient synthetic methods for the p...
2017, 37(6): 1352-1367
doi: 10.6023/cjoc201701027
Abstract:
Ruthenium and its complex possess various catalytic activities such as oxidation and reduction. Ruthenium as a cheap and efficient catalyst was also widely used in such field as C—H activation. Considerable attention has been paid to it for its great...
Ruthenium and its complex possess various catalytic activities such as oxidation and reduction. Ruthenium as a cheap and efficient catalyst was also widely used in such field as C—H activation. Considerable attention has been paid to it for its great...
2017, 37(6): 1368-1381
doi: 10.6023/cjoc201702010
Abstract:
Antimycin A is a class of natural products bearing a dilactone-ring moiety as the core skeleton. These compounds have been identified as specific inhibitors of the mitochondrial respiratory chain and bind to the Qi site of the cytochrome bc1 complex....
Antimycin A is a class of natural products bearing a dilactone-ring moiety as the core skeleton. These compounds have been identified as specific inhibitors of the mitochondrial respiratory chain and bind to the Qi site of the cytochrome bc1 complex....
2017, 37(6): 1382-1391
doi: 10.6023/cjoc201612031
Abstract:
C-Glycosides in which the interglycosidic oxygen atom have been replaced by carbon atom are widely found in natural products and drug molecules. They have better enzymatic and hydrolytic stablility compared to their corresponding O-glycosides and N-g...
C-Glycosides in which the interglycosidic oxygen atom have been replaced by carbon atom are widely found in natural products and drug molecules. They have better enzymatic and hydrolytic stablility compared to their corresponding O-glycosides and N-g...
2017, 37(6): 1392-1397
doi: 10.6023/cjoc201702047
Abstract:
A mononuclear cobalt(Ⅱ) complex[Co(4-MeOC6H4Se)2(PMe3)3] (1) and a dinuclear cobalt diphenylselenolato complex[Co(PMe3)2(SeC6H4-2-Me)]2 (2) were obtained from the reaction of 4-methoxyselenophenol and 2-methylseleno-phenol with Co(PMe3)4, respectivel...
A mononuclear cobalt(Ⅱ) complex[Co(4-MeOC6H4Se)2(PMe3)3] (1) and a dinuclear cobalt diphenylselenolato complex[Co(PMe3)2(SeC6H4-2-Me)]2 (2) were obtained from the reaction of 4-methoxyselenophenol and 2-methylseleno-phenol with Co(PMe3)4, respectivel...
2017, 37(6): 1407-1411
doi: 10.6023/cjoc201701040
Abstract:
Transfer hydrogenation is a mild and effective way in reduction reaction. In this paper, a simple approach of selectively hydrogenation of alkynes to cis-alkenes with NH2NH2·H2O as a transfer hydrogenation agent in the presence of air without any cat...
Transfer hydrogenation is a mild and effective way in reduction reaction. In this paper, a simple approach of selectively hydrogenation of alkynes to cis-alkenes with NH2NH2·H2O as a transfer hydrogenation agent in the presence of air without any cat...
2017, 37(6): 1412-1416
doi: 10.6023/cjoc201611037
Abstract:
Five novel ferrocenyl thiazole and imidazole derivatives were synthesized. The structure characterization of the five products showed that ferrocene conjugative unit and thiazole or imidazole conjugative unit were linked by carbonyl methylene skeleto...
Five novel ferrocenyl thiazole and imidazole derivatives were synthesized. The structure characterization of the five products showed that ferrocene conjugative unit and thiazole or imidazole conjugative unit were linked by carbonyl methylene skeleto...
2017, 37(6): 1417-1425
doi: 10.6023/cjoc201610033
Abstract:
By means of computer aided drug design, simulation of apoptosis inhibiting protein complex glycine receptor kinase C-kit docking with active small molecules. Ten analogues were successfully synthesized by the introduction of nitrogen-containing heter...
By means of computer aided drug design, simulation of apoptosis inhibiting protein complex glycine receptor kinase C-kit docking with active small molecules. Ten analogues were successfully synthesized by the introduction of nitrogen-containing heter...
2017, 37(6): 1426-1432
doi: 10.6023/cjoc201612037
Abstract:
2-O-(β-D-Glucopyranosyl)-L-ascorbic acid, a natural β-glycoside with ascorbic acid moiety present in Lycium barbarum, and its two analogues were chemically synthesized. Their inhibitory effect on yeast α-glucosidase and α-amylase were investigated wi...
2-O-(β-D-Glucopyranosyl)-L-ascorbic acid, a natural β-glycoside with ascorbic acid moiety present in Lycium barbarum, and its two analogues were chemically synthesized. Their inhibitory effect on yeast α-glucosidase and α-amylase were investigated wi...
2017, 37(6): 1433-1442
doi: 10.6023/cjoc201612038
Abstract:
A concise and environment friendly route for the synthesis of multisubstituted chromone-fused bicyclic pyridine compounds via one-step reaction of chromone-3-carboxaldehyde 1 and N-benzyl nitro ketene aminals (NBNKAs, 2) in ethanol media has been de...
A concise and environment friendly route for the synthesis of multisubstituted chromone-fused bicyclic pyridine compounds via one-step reaction of chromone-3-carboxaldehyde 1 and N-benzyl nitro ketene aminals (NBNKAs, 2) in ethanol media has been de...
2017, 37(6): 1443-1449
doi: 10.6023/cjoc201612056
Abstract:
A new Methoxy poly(ethylene glycol)-anchored polymer sensor P1, which contains anthracene fluorephore and di-2-picolylamine metal ions binding site, has been easily synthesized by "click reaction". In pure aqueous solution, P1 can coordinate with Hg2...
A new Methoxy poly(ethylene glycol)-anchored polymer sensor P1, which contains anthracene fluorephore and di-2-picolylamine metal ions binding site, has been easily synthesized by "click reaction". In pure aqueous solution, P1 can coordinate with Hg2...
2017, 37(6): 1450-1455
doi: 10.6023/cjoc201610030
Abstract:
The reaction of arylboronic acids with bismuth(Ⅲ) nitrate pentahydrate resulted in a series of nitroarenes when the reaction was carried out under microwave (120 ℃) for 1 min in 1, 2-dichloroethane. Compared with traditional heating condition, the me...
The reaction of arylboronic acids with bismuth(Ⅲ) nitrate pentahydrate resulted in a series of nitroarenes when the reaction was carried out under microwave (120 ℃) for 1 min in 1, 2-dichloroethane. Compared with traditional heating condition, the me...
2017, 37(6): 1456-1462
doi: 10.6023/cjoc201612034
Abstract:
1, 2-Dihexadecyl-sn-glycero-3-phosphoethanolamine (DHPE) is one type of glycerophospholipids, and it has a wide range of application in biology. A new and efficient method was developed to synthesis DHPE using (S)-2, 2-dimethyl-1, 3-dioxolane-4-metha...
1, 2-Dihexadecyl-sn-glycero-3-phosphoethanolamine (DHPE) is one type of glycerophospholipids, and it has a wide range of application in biology. A new and efficient method was developed to synthesis DHPE using (S)-2, 2-dimethyl-1, 3-dioxolane-4-metha...
2017, 37(6): 1463-1472
doi: 10.6023/cjoc201611005
Abstract:
A series of novel 3, 4-dihydro-benzo[b]oxazepin-5(2H)-one derivatives were designed and synthesized as potent protein-tyrosine kinases (PTKs, e.g. ErbB1, ErbB2, c-Met, ALK, FGFR1, RET, KDR) inhibitors. All compounds were characterized by NMR and MS. ...
A series of novel 3, 4-dihydro-benzo[b]oxazepin-5(2H)-one derivatives were designed and synthesized as potent protein-tyrosine kinases (PTKs, e.g. ErbB1, ErbB2, c-Met, ALK, FGFR1, RET, KDR) inhibitors. All compounds were characterized by NMR and MS. ...
2017, 37(6): 1473-1478
doi: 10.6023/cjoc201612047
Abstract:
An efficient synthesis of 2-vinyl furans and thiophenes through oxidative Heck reaction has been explored under solvent-less high-speed ball-milling conditions. This Pd-catalyzed oxidative Heck reaction proceeded well with both acrylates and styrenes...
An efficient synthesis of 2-vinyl furans and thiophenes through oxidative Heck reaction has been explored under solvent-less high-speed ball-milling conditions. This Pd-catalyzed oxidative Heck reaction proceeded well with both acrylates and styrenes...
2017, 37(6): 1479-1486
doi: 10.6023/cjoc201611031
Abstract:
A series of novel purin-8-one derivatives were prepared with the starting materials of 2, 4-dichloro-5-nitropyrimidine and followed by multi-step reactions. The structures of all target compounds were identified by 1H NMR, 13C NMR and HRMS. The preli...
A series of novel purin-8-one derivatives were prepared with the starting materials of 2, 4-dichloro-5-nitropyrimidine and followed by multi-step reactions. The structures of all target compounds were identified by 1H NMR, 13C NMR and HRMS. The preli...
2017, 37(6): 1487-1493
doi: 10.6023/cjoc201612029
Abstract:
A fast and efficient CuI-catalyzed intramolecular C—N coupling reaction of N-(2-bromoaryl)-1H-pyrazol-5-amines to synthesize benzo[4, 5]imidazo[1, 2-b]pyrazoles has been developed from N-(2-bromoaryl)-thioacetanilides. A series of benzo[4, 5]imidazo[...
A fast and efficient CuI-catalyzed intramolecular C—N coupling reaction of N-(2-bromoaryl)-1H-pyrazol-5-amines to synthesize benzo[4, 5]imidazo[1, 2-b]pyrazoles has been developed from N-(2-bromoaryl)-thioacetanilides. A series of benzo[4, 5]imidazo[...
2017, 37(6): 1494-1500
doi: 10.6023/cjoc201612035
Abstract:
This article describes the synthesis of warfarin and its derivatives by using the crude earthwarm extract as a biocatalyst. Warfarin, an effective anticogulant being used for half a century, has enormous clinic and commercial value. Warfarin and its ...
This article describes the synthesis of warfarin and its derivatives by using the crude earthwarm extract as a biocatalyst. Warfarin, an effective anticogulant being used for half a century, has enormous clinic and commercial value. Warfarin and its ...
2017, 37(6): 1501-1505
doi: 10.6023/cjoc201610031
Abstract:
The haloalkynes were hydrolyzed to α-haloketones by sulfuric acid promotion in ionic liquids (ILs) with 85%~94% yields. The ILs-H2SO4 reaction system could be easily recycled (more five times) without any effect for reaction yield. At the same time, ...
The haloalkynes were hydrolyzed to α-haloketones by sulfuric acid promotion in ionic liquids (ILs) with 85%~94% yields. The ILs-H2SO4 reaction system could be easily recycled (more five times) without any effect for reaction yield. At the same time, ...
2017, 37(6): 1506-1515
doi: 10.6023/cjoc201610043
Abstract:
A series of novel hybrid compounds between indolo[b]tetrahydrofuran and imidazolium salts were prepared from tryptophol by four steps of Sharpless epoxidation, amidation, coupling and salt formation. Their structures were confirmed by 1H NMR, 13C NMR...
A series of novel hybrid compounds between indolo[b]tetrahydrofuran and imidazolium salts were prepared from tryptophol by four steps of Sharpless epoxidation, amidation, coupling and salt formation. Their structures were confirmed by 1H NMR, 13C NMR...
2017, 37(6): 1516-1522
doi: 10.6023/cjoc201612012
Abstract:
As the active component in visci herba of traditional Chinese medicine, homoeriodictyol-7-O-β-D-glycoside has been widely studied for years. In this paper, the first synthesis of homoeriodictyol-7-O-β-D-glycoside and its diastereoisomer has been achi...
As the active component in visci herba of traditional Chinese medicine, homoeriodictyol-7-O-β-D-glycoside has been widely studied for years. In this paper, the first synthesis of homoeriodictyol-7-O-β-D-glycoside and its diastereoisomer has been achi...
2017, 37(6): 1398-1406
doi: 10.6023/cjoc201701020
Abstract:
A chiral prosthetic group induced heterogeneous diastereoselective asymmetric hydrogenation of β-dehydroamino esters, catalyzed by Pt/Al2O3, has been developed. A series of β-dehydroamino esters were successfully hydrogenated in high yields with good...
A chiral prosthetic group induced heterogeneous diastereoselective asymmetric hydrogenation of β-dehydroamino esters, catalyzed by Pt/Al2O3, has been developed. A series of β-dehydroamino esters were successfully hydrogenated in high yields with good...
2017, 37(6): 1523-1529
doi: 10.6023/cjoc201704018
Abstract:
Acute myelogenous leukemia is a malignant disease of the hemopoietic tissue, which causes great harm to human health, and there is no therapeutic drugs with low toxicity and high efficiency. Indirubin is the active constituent of the traditional chin...
Acute myelogenous leukemia is a malignant disease of the hemopoietic tissue, which causes great harm to human health, and there is no therapeutic drugs with low toxicity and high efficiency. Indirubin is the active constituent of the traditional chin...
2017, 37(6): 1530-1536
doi: 10.6023/cjoc201703006
Abstract:
Pseudoginsenoside HQ[PHQ, 3β-O-β-D-glucopyranosyl-(20S, 24S)-epoxydammarane-12β, 25-diol] is the main in vivo metabolite of 20(S)-ginsenoside Rh2 which has high biological activities, with potential medicinal value. The reported chemical synthesis of...
Pseudoginsenoside HQ[PHQ, 3β-O-β-D-glucopyranosyl-(20S, 24S)-epoxydammarane-12β, 25-diol] is the main in vivo metabolite of 20(S)-ginsenoside Rh2 which has high biological activities, with potential medicinal value. The reported chemical synthesis of...
2017, 37(6): 1537-1541
doi: 10.6023/cjoc201701009
Abstract:
To search for the pyridine pesticide lead compound with high antigungal activity, a series of novel 3-phenyl propan-1-one oxime ethers bearing pyridine moiety were synthesized using 3-acetypyridine, benzaldehyde, substituted anilines and alkoxyamine ...
To search for the pyridine pesticide lead compound with high antigungal activity, a series of novel 3-phenyl propan-1-one oxime ethers bearing pyridine moiety were synthesized using 3-acetypyridine, benzaldehyde, substituted anilines and alkoxyamine ...
2017, 37(6): 1542-1547
doi: 10.6023/cjoc201701042
Abstract:
In order to explore novel pyrazole derivatives with good biological activities, a series of novel pyrazole oxime ester compounds containing pyridyl moiety were designed and synthesized according to the method of active substructure combination. The s...
In order to explore novel pyrazole derivatives with good biological activities, a series of novel pyrazole oxime ester compounds containing pyridyl moiety were designed and synthesized according to the method of active substructure combination. The s...
2017, 37(6): 1548-1555
doi: 10.6023/cjoc201612001
Abstract:
An efficient method for the synthesis of pyrano[3, 2-c]quinoline-4, 5-dione derivatives via iodine promoted intramolecular cyclization of 1-methyl-3-cinnamoyl-4-hydroxyquinolin-2-one, synthesized from aldol condensation of 1-methyl-3-acetyl-4-hydroxy...
An efficient method for the synthesis of pyrano[3, 2-c]quinoline-4, 5-dione derivatives via iodine promoted intramolecular cyclization of 1-methyl-3-cinnamoyl-4-hydroxyquinolin-2-one, synthesized from aldol condensation of 1-methyl-3-acetyl-4-hydroxy...
2017, 37(6): 1560-1564
doi: 10.6023/cjoc201612044
Abstract:
Six kinds of 5, 5-(phenylmethylene)bis(2, 2-dimethyl-1, 3-dioxane-4, 6-dione) derivatives were synthesized by the reaction of aromatic aldehydes and 2, 2-dimethyl-1, 3-dioxane-4, 6-dione in biobased gluconic acid aqueous solution at 40 ℃. The reactio...
Six kinds of 5, 5-(phenylmethylene)bis(2, 2-dimethyl-1, 3-dioxane-4, 6-dione) derivatives were synthesized by the reaction of aromatic aldehydes and 2, 2-dimethyl-1, 3-dioxane-4, 6-dione in biobased gluconic acid aqueous solution at 40 ℃. The reactio...
2017, 37(6): 1565-1570
doi: 10.6023/cjoc201608020
Abstract:
A series of 11-aryl-8, 11-dihydrofuro[3', 4':5, 6]pyrido[3, 2-f]quinoxalin-10(7H)-one derivatives were obtained via a one-pot and three-component reaction of aromatic aldehydes, 6-aminoquinoxaline and tetronic acid in EtOH. The structure of 11-(4-nit...
A series of 11-aryl-8, 11-dihydrofuro[3', 4':5, 6]pyrido[3, 2-f]quinoxalin-10(7H)-one derivatives were obtained via a one-pot and three-component reaction of aromatic aldehydes, 6-aminoquinoxaline and tetronic acid in EtOH. The structure of 11-(4-nit...
2017, 37(6): 1571-1576
doi: 10.6023/cjoc201611018
Abstract:
A useful strategy for the synthesis of enol phosphates from β-keto esters via Atherton-Atodd reaction was developed. A variety of enol phosphates can be quickly and readily prepared with broad substrate scope and moderate yields under mild conditions...
A useful strategy for the synthesis of enol phosphates from β-keto esters via Atherton-Atodd reaction was developed. A variety of enol phosphates can be quickly and readily prepared with broad substrate scope and moderate yields under mild conditions...
2017, 37(6): 1556-1559
doi: 10.6023/cjoc201612003
Abstract:
The C—S cross-coupling of aryl halides with alkyl thiols under transition metal-free conditions was investigated. Good to excellent yields can be obtained for a variety of electron-poor aryl halides with alkyl thiols in the presence of KOtBu even at ...
The C—S cross-coupling of aryl halides with alkyl thiols under transition metal-free conditions was investigated. Good to excellent yields can be obtained for a variety of electron-poor aryl halides with alkyl thiols in the presence of KOtBu even at ...
2017, 37(6): 1577-1581
doi: 10.6023/cjoc201701016
Abstract:
Four new closely related vicinal diols, (1R, 2R)-1-(5-(pent-4-en-1-yl)furan-2-yl)propane-1, 2-diol (1), (1S, 2R)-1-(5-(pent-4-en-1-yl)furan-2-yl)propane-1, 2-diol (2), (1R, 2R)-1-(5-pentylfuran-2-yl)propane-1, 2-diol (3) and (1R, 2S)-1-(5-pen-tylfura...
Four new closely related vicinal diols, (1R, 2R)-1-(5-(pent-4-en-1-yl)furan-2-yl)propane-1, 2-diol (1), (1S, 2R)-1-(5-(pent-4-en-1-yl)furan-2-yl)propane-1, 2-diol (2), (1R, 2R)-1-(5-pentylfuran-2-yl)propane-1, 2-diol (3) and (1R, 2S)-1-(5-pen-tylfura...
2017, 37(6): 1582-1584
doi: 10.6023/cjoc201701035
Abstract:
A practical synthesis of trifluoromethanesulfonate esters by reaction of orthoformate esters with triflic anhydride is described. The solvent-free method featured mild condition, short time, high yield, simple operation and broad substrate scope. The...
A practical synthesis of trifluoromethanesulfonate esters by reaction of orthoformate esters with triflic anhydride is described. The solvent-free method featured mild condition, short time, high yield, simple operation and broad substrate scope. The...
