Catalyzed by ytterbium(III) triflate hydrate [Yb(OTf)3.xH20], the Michael addition and cyclocondensation of α,β-unsaturated ketones with active methylene compounds to afford the 1,4-adducts and benzo[b]pyran der...Catalyzed by ytterbium(III) triflate hydrate [Yb(OTf)3.xH20], the Michael addition and cyclocondensation of α,β-unsaturated ketones with active methylene compounds to afford the 1,4-adducts and benzo[b]pyran derivatives, respectively were studied.展开更多
The reactions of tri-2-benzofuranylborane or aminoethyl di-2-thienylborinate and 2-thienylphenylborinate with dichlorocarbene generated in situ from chloroform under phase transfer conditions were explored as a new ro...The reactions of tri-2-benzofuranylborane or aminoethyl di-2-thienylborinate and 2-thienylphenylborinate with dichlorocarbene generated in situ from chloroform under phase transfer conditions were explored as a new route for the preparation of heteroaromatic ketones. It was found that a good yield of the ketones can be obtained by solid-liquid system.展开更多
Cerium trichloride heptahydrate(CeCl_3·7H_2O) was found to be an efficient and recyclable catalyst for the three-component direct Mannich reaction of anilines and benzaldehydes with acetophenone.This protocol has...Cerium trichloride heptahydrate(CeCl_3·7H_2O) was found to be an efficient and recyclable catalyst for the three-component direct Mannich reaction of anilines and benzaldehydes with acetophenone.This protocol has advantages of high yield,no environmental pollution,mild condition,and simple work-up procedure.展开更多
Regio and stereoselective synthesis of substituted dihydrofurans were accomplished by eeric ammonium nitrate mediated oxidative cycloaddition of 1,3-dicarbonyls to β-aryl-α,β-unsaturated ketones in moderate yields.
We report a new, effective and simple method for preparing a,fl-unsaturated carbonyl compounds by reacting ketones and aromatic alcohols at 56 ℃ in the presence of CrO3 (CrO3 acts as an oxidant and also a catalyst)...We report a new, effective and simple method for preparing a,fl-unsaturated carbonyl compounds by reacting ketones and aromatic alcohols at 56 ℃ in the presence of CrO3 (CrO3 acts as an oxidant and also a catalyst) for around 10 h. The condensation reactions occurred effectively among a wide combination of ketones and alcohols. The procedure is simple and the yields can be high up to 98%. And a probable mechanism is proposed.展开更多
A novel Dendritic Compound (2) of triphenylene- 2,6,10-trione ketal-tri-{2,2-di-[(N-methyl-N-(4-py- ridinyl) amino)methyl]-1,3-propanediol} was conveniently synthesized by aromatization of cyclohexanedione mono-ketal,...A novel Dendritic Compound (2) of triphenylene- 2,6,10-trione ketal-tri-{2,2-di-[(N-methyl-N-(4-py- ridinyl) amino)methyl]-1,3-propanediol} was conveniently synthesized by aromatization of cyclohexanedione mono-ketal, ketal-exchange reaction with 2,2-dibromomethyl-1,3-propane- diol and nuclophilic substitution with N-methy- laminopyridine as nuclophilic reagent. The Mo-rita-Baylis-Hillman reaction of various aryl al-dehydes with methyl vinyl ketone and acryloni-trile in (DMF/cyclohexane, 1/1, v/v) has been investigated by using Dendritic Compound (2) as catalyst. The corresponding Morita-Baylis- Hillman adducts was obtained in good yields by using the recycled and reactivated dendritic catalyst.展开更多
This paper presents the results of the search of biologically active uranium compounds such as amino acids. We first received and examined X-ray and IR (infrared radiation) spectroscopy of uranium complexes with α-...This paper presents the results of the search of biologically active uranium compounds such as amino acids. We first received and examined X-ray and IR (infrared radiation) spectroscopy of uranium complexes with α- and β-amino acids in aqueous and organic solution. We proposed a method for direct synthesis of complex organic compounds of uranium chloride UO2Cl2 with α- andβ-amino acids for the synthesis of drugs for the treatment of cancer.展开更多
The intermolecular reductive cyclization of o-nitrobenzene-sulfonamides with aliphatic ketones induced by TiCl4/Sm system was studied and a series of 3, 3-disubstituted-3,4-dihydro(2H)-1,2, 4-benzothiadiazine-1,1-diox...The intermolecular reductive cyclization of o-nitrobenzene-sulfonamides with aliphatic ketones induced by TiCl4/Sm system was studied and a series of 3, 3-disubstituted-3,4-dihydro(2H)-1,2, 4-benzothiadiazine-1,1-dioxides were synthesized in moderate to high yields under mild and neutral conditions.展开更多
The synthesis of two series of [3-amino ketones containing a p-aminobenzoic acid moiety (TM.1 and TM-2) using a modified protocol of the Mannich reaction is reported. The molecular structures of a total of tweenty t...The synthesis of two series of [3-amino ketones containing a p-aminobenzoic acid moiety (TM.1 and TM-2) using a modified protocol of the Mannich reaction is reported. The molecular structures of a total of tweenty three new target compounds were characterized by ~H NMR, 1~C NMR, ESI-MS and HR-MS. Subsequently, their antidiabetic activities were screened in vitro. The c^-glucodase inhibition (c^-GI) activity of compound le reached a remarkable level of 66.50%. The peroxisome proliferator- activated receptor (PPAR) relative activation activities of six compounds are above 80%, and in particular 2i displays an un- precedentedly high PPAR of 130.91%. The structure-activity relationships of the compounds were established. 2i is also sub- ject to further in-depth investigation.展开更多
Sulfuric acid-modified polyethylene glycol 6000(PEG-OSO_3H) was applied as an efficient and recyclable catalyst for the synthesis ofβ-amino carbonyl compounds via the Mannich reaction between aldehydes,aromatic ket...Sulfuric acid-modified polyethylene glycol 6000(PEG-OSO_3H) was applied as an efficient and recyclable catalyst for the synthesis ofβ-amino carbonyl compounds via the Mannich reaction between aldehydes,aromatic ketones and aromatic amines at room temperature using PEG400-H_2O(1:1) as environment-friendly solvents.The reactions were completed in short times and mild reaction conditions with good to excellent yields.展开更多
Saccharose was applied as an efficient and homogenous catalyst for a one-pot,three-component Mannich reaction for the formation ofβ-aminoketones from aromatic aldehydes,anilines,and acetophenone at ambient temperatur...Saccharose was applied as an efficient and homogenous catalyst for a one-pot,three-component Mannich reaction for the formation ofβ-aminoketones from aromatic aldehydes,anilines,and acetophenone at ambient temperature in excellent yields.This protocol has the following advantages: mild conditions,high yields,clean reaction profiles,operational simplicity,and environmentally benign and simple work-up procedures.展开更多
A facile transformation of alkynes into α-amino ketones by an N-bromosuccinimide-mediated one-pot cascade strategy is described. A variety of α-amino ketones are obtained in moderate to good yields under mild condit...A facile transformation of alkynes into α-amino ketones by an N-bromosuccinimide-mediated one-pot cascade strategy is described. A variety of α-amino ketones are obtained in moderate to good yields under mild conditions. To overcome the multi-step synthesis, N-bromosuccinimide is involved in multiple tasks, playing a key role in the reaction course.展开更多
Mannich reactions of imine with acetylacetone were effectively catalyzed by the modified chiral cinchona alka-loid-derived thiourea. The reactions led to chiral r-amino carbonyl compounds in high yields and good enant...Mannich reactions of imine with acetylacetone were effectively catalyzed by the modified chiral cinchona alka-loid-derived thiourea. The reactions led to chiral r-amino carbonyl compounds in high yields and good enantiose-lectivities. The study demonstrated for the first time that Mannich reactions of unmodified acetylacetone with het-erocyclic imine derived from benzothiazole can be promoted by chiral bifunctional organocatalyst.展开更多
The easily prepared and recoverable chiral N-sulfonylated fl-amino alcohol 2 in combination with Ti(OPr-i)4 was found to be an effective chiral catalyst for the enantioselective addition of alkynylzinc to ketones, w...The easily prepared and recoverable chiral N-sulfonylated fl-amino alcohol 2 in combination with Ti(OPr-i)4 was found to be an effective chiral catalyst for the enantioselective addition of alkynylzinc to ketones, which gave the useful products, i.e. chiral tertiary propargyl alcohols, with the ee up to 92%.展开更多
基金the National Natural Science Foundation of China (No.20676123) for financial support.
文摘Catalyzed by ytterbium(III) triflate hydrate [Yb(OTf)3.xH20], the Michael addition and cyclocondensation of α,β-unsaturated ketones with active methylene compounds to afford the 1,4-adducts and benzo[b]pyran derivatives, respectively were studied.
文摘The reactions of tri-2-benzofuranylborane or aminoethyl di-2-thienylborinate and 2-thienylphenylborinate with dichlorocarbene generated in situ from chloroform under phase transfer conditions were explored as a new route for the preparation of heteroaromatic ketones. It was found that a good yield of the ketones can be obtained by solid-liquid system.
基金the financial support from Nanjing University of Science and Technology.
文摘Cerium trichloride heptahydrate(CeCl_3·7H_2O) was found to be an efficient and recyclable catalyst for the three-component direct Mannich reaction of anilines and benzaldehydes with acetophenone.This protocol has advantages of high yield,no environmental pollution,mild condition,and simple work-up procedure.
文摘Regio and stereoselective synthesis of substituted dihydrofurans were accomplished by eeric ammonium nitrate mediated oxidative cycloaddition of 1,3-dicarbonyls to β-aryl-α,β-unsaturated ketones in moderate yields.
基金Project supported by the National Natural Science Foundation of China (NSFC) (Nos. 50825303 and 30890140) and the Ministry of Science and Technology of China (No. 2009CB-930400).
文摘We report a new, effective and simple method for preparing a,fl-unsaturated carbonyl compounds by reacting ketones and aromatic alcohols at 56 ℃ in the presence of CrO3 (CrO3 acts as an oxidant and also a catalyst) for around 10 h. The condensation reactions occurred effectively among a wide combination of ketones and alcohols. The procedure is simple and the yields can be high up to 98%. And a probable mechanism is proposed.
文摘A novel Dendritic Compound (2) of triphenylene- 2,6,10-trione ketal-tri-{2,2-di-[(N-methyl-N-(4-py- ridinyl) amino)methyl]-1,3-propanediol} was conveniently synthesized by aromatization of cyclohexanedione mono-ketal, ketal-exchange reaction with 2,2-dibromomethyl-1,3-propane- diol and nuclophilic substitution with N-methy- laminopyridine as nuclophilic reagent. The Mo-rita-Baylis-Hillman reaction of various aryl al-dehydes with methyl vinyl ketone and acryloni-trile in (DMF/cyclohexane, 1/1, v/v) has been investigated by using Dendritic Compound (2) as catalyst. The corresponding Morita-Baylis- Hillman adducts was obtained in good yields by using the recycled and reactivated dendritic catalyst.
文摘This paper presents the results of the search of biologically active uranium compounds such as amino acids. We first received and examined X-ray and IR (infrared radiation) spectroscopy of uranium complexes with α- and β-amino acids in aqueous and organic solution. We proposed a method for direct synthesis of complex organic compounds of uranium chloride UO2Cl2 with α- andβ-amino acids for the synthesis of drugs for the treatment of cancer.
基金Project supported by the National Natural Science Foundation of China (No. 29872010)Natural Science Foundation of Zhejiang Province, China
文摘The intermolecular reductive cyclization of o-nitrobenzene-sulfonamides with aliphatic ketones induced by TiCl4/Sm system was studied and a series of 3, 3-disubstituted-3,4-dihydro(2H)-1,2, 4-benzothiadiazine-1,1-dioxides were synthesized in moderate to high yields under mild and neutral conditions.
基金the Natural Science Foundation of Chongqing (2005BB5095)the Ph.D Research Foundation of Southwest University (SWNU, B2005010)the Scientific and Technological Project in Chongqing (CSTC, 2011AB5001) for financial support
文摘The synthesis of two series of [3-amino ketones containing a p-aminobenzoic acid moiety (TM.1 and TM-2) using a modified protocol of the Mannich reaction is reported. The molecular structures of a total of tweenty three new target compounds were characterized by ~H NMR, 1~C NMR, ESI-MS and HR-MS. Subsequently, their antidiabetic activities were screened in vitro. The c^-glucodase inhibition (c^-GI) activity of compound le reached a remarkable level of 66.50%. The peroxisome proliferator- activated receptor (PPAR) relative activation activities of six compounds are above 80%, and in particular 2i displays an un- precedentedly high PPAR of 130.91%. The structure-activity relationships of the compounds were established. 2i is also sub- ject to further in-depth investigation.
基金the financial support from the National Natural Science Foundation of China(Nos.20902073 and 21062017)the Natural Science Foundation of Gansu Province(No.096RJZA116)the Scientific and Technological Innovation Engineering program of Northwest Normal University(Nos.nwnu-kjcxgc-03-64,nwnulkqn -10-15)
文摘Sulfuric acid-modified polyethylene glycol 6000(PEG-OSO_3H) was applied as an efficient and recyclable catalyst for the synthesis ofβ-amino carbonyl compounds via the Mannich reaction between aldehydes,aromatic ketones and aromatic amines at room temperature using PEG400-H_2O(1:1) as environment-friendly solvents.The reactions were completed in short times and mild reaction conditions with good to excellent yields.
基金financial support from the Research Council of University of Sistan and Baluchestan
文摘Saccharose was applied as an efficient and homogenous catalyst for a one-pot,three-component Mannich reaction for the formation ofβ-aminoketones from aromatic aldehydes,anilines,and acetophenone at ambient temperature in excellent yields.This protocol has the following advantages: mild conditions,high yields,clean reaction profiles,operational simplicity,and environmentally benign and simple work-up procedures.
基金the Natural Science Foundation of Xinjiang Province(No. 2016D01C009)the Educational Commission of Xinjiang(No. XJEDU2017S053)for financial support
文摘A facile transformation of alkynes into α-amino ketones by an N-bromosuccinimide-mediated one-pot cascade strategy is described. A variety of α-amino ketones are obtained in moderate to good yields under mild conditions. To overcome the multi-step synthesis, N-bromosuccinimide is involved in multiple tasks, playing a key role in the reaction course.
基金Project supported by the National Key Project for Basic Research (No. 2010CB126105), Key Technologies R&D Program (No. 2011BAE06B05), the National Natural Science Foundation of China (No. 20872021) and Innovation Foundation for Graduate Students in Guizhou University (No. 2010023).
文摘Mannich reactions of imine with acetylacetone were effectively catalyzed by the modified chiral cinchona alka-loid-derived thiourea. The reactions led to chiral r-amino carbonyl compounds in high yields and good enantiose-lectivities. The study demonstrated for the first time that Mannich reactions of unmodified acetylacetone with het-erocyclic imine derived from benzothiazole can be promoted by chiral bifunctional organocatalyst.
基金Project supported by the National Natural Science Foundation of China (Nos. 29925205, 30271488, 20021001 and 203900501).
文摘The easily prepared and recoverable chiral N-sulfonylated fl-amino alcohol 2 in combination with Ti(OPr-i)4 was found to be an effective chiral catalyst for the enantioselective addition of alkynylzinc to ketones, which gave the useful products, i.e. chiral tertiary propargyl alcohols, with the ee up to 92%.