4,6-Diarylpyrimidin-2(1H)-one derivatives have been synthesized from three-component one-pot condensation of acetophe-none derivatives,aldehydes and urea in the presence of trimethylsilyl chloride and a catalytic amou...4,6-Diarylpyrimidin-2(1H)-one derivatives have been synthesized from three-component one-pot condensation of acetophe-none derivatives,aldehydes and urea in the presence of trimethylsilyl chloride and a catalytic amount of HPMoOunder solvent-free conditions.展开更多
A novel approach to the synthesis of 6, 7-disubstituted-1H-quinoxalin-2-ones is described.The title compounds were regioselectively prepared by starting from substituted phenylamines andchloroacetyl chloride through t...A novel approach to the synthesis of 6, 7-disubstituted-1H-quinoxalin-2-ones is described.The title compounds were regioselectively prepared by starting from substituted phenylamines andchloroacetyl chloride through the efficient sequence of acylation, nitration, reduction, intramolecular alkylation, and oxidation.展开更多
Heteropoly acids efficiently catalyzed the cyclocondensation reaction of anthranilamide with aldehydes in water at ambient temperature and afforded the corresponding 2,3-dihydro-4(1H)-quinazolinones compounds in goo...Heteropoly acids efficiently catalyzed the cyclocondensation reaction of anthranilamide with aldehydes in water at ambient temperature and afforded the corresponding 2,3-dihydro-4(1H)-quinazolinones compounds in good to excellent yields.This method provides mild reaction conditions and clean reaction profiles,using a small quantity of catalyst and a simple workup procedure.展开更多
The photo-/electrocatalytic functionalization of quinoxalin-2(1H)-ones has emerged as a promising and powerful approach for post-synthetic modification of quinoxalin-2(1H)-ones.This review provides an overview of rece...The photo-/electrocatalytic functionalization of quinoxalin-2(1H)-ones has emerged as a promising and powerful approach for post-synthetic modification of quinoxalin-2(1H)-ones.This review provides an overview of recent developments in photo-/electrocatalytic functionalization of quinoxalin-2(1H)-ones including arylation,alkylation,fluoroalkylation,amination,phosphorylation,acylation,alkoxylation,thiolation,silylation,and annulation.The reaction scope and the related mechanism are also well discussed.展开更多
Silica-supported tin chloride and titanium tetrachloride were prepared by the reaction of tin chloride and titanium tetrachloride with activated silica gel in refluxing toluene.These solid acids have been employed as ...Silica-supported tin chloride and titanium tetrachloride were prepared by the reaction of tin chloride and titanium tetrachloride with activated silica gel in refluxing toluene.These solid acids have been employed as the catalysts for the synthesis of bisdihydropyrimidin -2(1H)-ones from aromatic dialdehydes,1,3-dicarbonyl compounds and urea at 90℃under solvent-free conditions.展开更多
An efficient and practical route to various 3-alkoxylquinoxalin-2(1 H)-ones through visible-light photocatalytic C(sp^2)-H/O-H cross-dehydrogenation coupling of quinoxalin-2(1 H)-ones and alcohols,employing ambient ai...An efficient and practical route to various 3-alkoxylquinoxalin-2(1 H)-ones through visible-light photocatalytic C(sp^2)-H/O-H cross-dehydrogenation coupling of quinoxalin-2(1 H)-ones and alcohols,employing ambient air as an oxidant at room temperature under metal-free conditions,was developed.展开更多
A method of synthesis of 4,6-disubstituted 5-thioxo-1,2,4-triazin- 3-ones from benzothioformanilides and semicarbazide is described.And six new compounds were synthesized by this method.
The mass spectrometric fragmentation of 2a,4-disubstituted 5-benzoyl-2a,3,4,5-tetrahydro-2-phenoxy-azeto{[1,2-a]}[1,5]benzodiazepin-1(2H)-ones has been investigated by means of mass-analyzed ion kinetic energy spectro...The mass spectrometric fragmentation of 2a,4-disubstituted 5-benzoyl-2a,3,4,5-tetrahydro-2-phenoxy-azeto{[1,2-a]}[1,5]benzodiazepin-1(2H)-ones has been investigated by means of mass-analyzed ion kinetic energy spectrometry under electron impact ionization conditions. All compounds tend to lose different moieties, such as phenoxy, phenoxy and H, and phenoxyketene. Both [M +-PhO] and [M +-PhOH] ions could further lose CO, and the [M +-PhOCHCO] ions could lose propene or styrene, PhCON, PhCOHN, and other fragments.展开更多
A series of 2,4,5-triaryl substituted 1H-pyrazol-3(2H)-ones,as ALK5 inhibitors,were desigened,synthesized and evaluated in vitro.Most compounds exhibited noticeable ALK5 inhibition activities at 1μmol/L and display...A series of 2,4,5-triaryl substituted 1H-pyrazol-3(2H)-ones,as ALK5 inhibitors,were desigened,synthesized and evaluated in vitro.Most compounds exhibited noticeable ALK5 inhibition activities at 1μmol/L and displayed no significant cytotoxicities at 30μmol/L.展开更多
基金Islamic Azad University of Khorram Abad Council for the financial support
文摘4,6-Diarylpyrimidin-2(1H)-one derivatives have been synthesized from three-component one-pot condensation of acetophe-none derivatives,aldehydes and urea in the presence of trimethylsilyl chloride and a catalytic amount of HPMoOunder solvent-free conditions.
文摘A novel approach to the synthesis of 6, 7-disubstituted-1H-quinoxalin-2-ones is described.The title compounds were regioselectively prepared by starting from substituted phenylamines andchloroacetyl chloride through the efficient sequence of acylation, nitration, reduction, intramolecular alkylation, and oxidation.
基金the financial support of Key Laboratory of Resources and Environment Chemistry of West China(No.XZ0704).
文摘Heteropoly acids efficiently catalyzed the cyclocondensation reaction of anthranilamide with aldehydes in water at ambient temperature and afforded the corresponding 2,3-dihydro-4(1H)-quinazolinones compounds in good to excellent yields.This method provides mild reaction conditions and clean reaction profiles,using a small quantity of catalyst and a simple workup procedure.
文摘The photo-/electrocatalytic functionalization of quinoxalin-2(1H)-ones has emerged as a promising and powerful approach for post-synthetic modification of quinoxalin-2(1H)-ones.This review provides an overview of recent developments in photo-/electrocatalytic functionalization of quinoxalin-2(1H)-ones including arylation,alkylation,fluoroalkylation,amination,phosphorylation,acylation,alkoxylation,thiolation,silylation,and annulation.The reaction scope and the related mechanism are also well discussed.
文摘Silica-supported tin chloride and titanium tetrachloride were prepared by the reaction of tin chloride and titanium tetrachloride with activated silica gel in refluxing toluene.These solid acids have been employed as the catalysts for the synthesis of bisdihydropyrimidin -2(1H)-ones from aromatic dialdehydes,1,3-dicarbonyl compounds and urea at 90℃under solvent-free conditions.
文摘An efficient and practical route to various 3-alkoxylquinoxalin-2(1 H)-ones through visible-light photocatalytic C(sp^2)-H/O-H cross-dehydrogenation coupling of quinoxalin-2(1 H)-ones and alcohols,employing ambient air as an oxidant at room temperature under metal-free conditions,was developed.
文摘A method of synthesis of 4,6-disubstituted 5-thioxo-1,2,4-triazin- 3-ones from benzothioformanilides and semicarbazide is described.And six new compounds were synthesized by this method.
文摘The mass spectrometric fragmentation of 2a,4-disubstituted 5-benzoyl-2a,3,4,5-tetrahydro-2-phenoxy-azeto{[1,2-a]}[1,5]benzodiazepin-1(2H)-ones has been investigated by means of mass-analyzed ion kinetic energy spectrometry under electron impact ionization conditions. All compounds tend to lose different moieties, such as phenoxy, phenoxy and H, and phenoxyketene. Both [M +-PhO] and [M +-PhOH] ions could further lose CO, and the [M +-PhOCHCO] ions could lose propene or styrene, PhCON, PhCOHN, and other fragments.
文摘A series of 2,4,5-triaryl substituted 1H-pyrazol-3(2H)-ones,as ALK5 inhibitors,were desigened,synthesized and evaluated in vitro.Most compounds exhibited noticeable ALK5 inhibition activities at 1μmol/L and displayed no significant cytotoxicities at 30μmol/L.