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1Synthesis of a highly hydrophobic cyclic decapeptide by solid-phase synthesis of linear peptide and cyclization in solution显示文摘A general method was described to synthesize a highly hydrophobic cyclic peptide,cyclo[LWLWLWLWLQ]where underlines indicate D-configuration of the amino acid,by a two-step solid-phase/solution synthesis strategy.The linear decapeptide was assembled by standard Boc chemistry on solid-phase and subsequently cyclized in solution with high efficiency and reproducibility. In subsequent purification by semi-preparative HPLC,50%(v/v) DMF/H_2O was employed as the solvent to overcome the difficulty of solubilizat...Chen, Jian Zhang, Bei Xie, Cao Lu, Yi Wu, Wei 2010Chinese Chemical Letters2010,21,4:5
2STUDIES ON THE PRENYLFLAVONOIDS PART V.SYNTHESIS OF(±)LESPEDEZAFLAVANONE D显示文摘(±)Lespedezaflavanone D,8,5’-di(γ,γ-dimethylallyl)-5,7,2’,4’-tetrahydroxyflavanone,hasbeen synthesized by the condensation of 4,6-dimethoxymethoxy-3-(γ,γ-dimethylallyl)-2-hydroxy-acetophenone with 2,4-dimethoxymethoxy-5-(γ,γ-dimethylallyl)benzaldehydc followed by cyclization anddemethoxymethylation.Fang Jie ZHANG Hua Wu SHAO Yu Lin LI Satate key Laboratory of Applied Organic Chemistry,Lanzhou University,Lanzhou 730000 1993Chinese Chemical Letters1993,4,4:4
3Syntheses and properties of new herbicidal 2-arylthio-1 ,2,4-triazolo[1,5-a] pyrimidine derivatives显示文摘In search of novel herbicides with high activity, a series of 2-arylthio-1,2,4- triazolo [1, 5-a ] pyrimidines (3) were synthesized by cyclization of 5-amino-3-arylthio-1,2,4-triazoles with 1,3-diketones or by the nucleophilic substitution of substituted thiophenols with 2-methylsulfonyl-1, 2, 4-triazolo [ 1, 5-a]-pyrimidine. The structures of all compounds prepared were confirmed by 1H NMR and MS spectroscopy along with elemental analyses. Preliminary bioassays indicated that some of the compounds 3 had good herbicidal activity against rape. In addition, the regioselectivity in the reaction of 5-amino-3-sub-stituted arylthio-1,2,4-triazoles with benzoylacetone was studied.杨光富 陆荣键 费学宁 杨华铮 2000Chinese Journal of Chemistry2000,18,3:3
4Rhodium-catalyzed selective[2+2+2]cyclizations of 1,6-diynes with monoynes leading to isoindolines and isobenzofurans显示文摘A highly efficient and selective[2+2+2]cyclization of diynes and monoalkynes was catalyzed by rhodium under room temperature in water/THF mixed solvent,affording isoindolines and isobenzofurans in good to excellent yields.The center atoms (N,O) in the diynes showed a significant effect for the cyclization.Wu, Wei Zhang, Xiao Yun Kang, Shou Xing 2010Chinese Chemical Letters2010,21,1:2
5Synthesis of Phenanthridine and Quinoxaline Derivatives via Copper-Catalyzed Radical Cyanoalkylation of Cyclobutanone Oxime Esters and Vinyl Azides显示文摘Main observation and conclusion A copper-catalyzed radical cyclization of cyclobutanone oxime esters and vinyl azide is described.This method provides facile access to cyanoalkyl-substituted phenanthridines and quinoxalines with excellent isolated yields.Moreover,these reactions proceed under mild conditions with a board substrate scope and excellent functional group tolerance.Qi Liang Long Lin Guodong Li Xianqiang Kong Bo Xu 2021Chinese Journal of Chemistry2021,39,7:2
6NaBAr^F4-Catalyzed Oxidative Cyclization of 1,5-and 1,6-Diynes:Efficient and Divergent Synthesis of Functionalized γ-and δ-Lactams显示文摘Summary of main observation and conclusion An efficient NaBAr^F4-catalyzed oxidative cyclization of readily available 1,5-and 1,6-diynes has been developed.Importantly,this transition metal-free oxidative catalysis proceeds via a presumable Lewis acid-catalyzed SN2′pathway,which is distinct from the relevant oxidative rhodium and gold catalysis.This method leads to the facile and practical construction of a diverse range of synthetically useful γ- and δ-lactams in mostly good to excellent yields with broad substrate scope.Bo-Han Zhu Cai-Ming Wang Hong-Yu Su Long-Wu Ye 2019Chinese Journal of Chemistry2019,37,1:2
7Studies on macrocyclic diterpenoids Ⅴ.Synthesis of(±)-sarcophytol-A benzyl ether显示文摘The title compound,sarcophytol-A benzyl ether has been synthesized through 13 stepsby employing acetone and geraniol as starting materials.The key steps in the synthesis weredouble bond migration reaction of allylic alcohols 5 and 6,phase transfer catalytic coupling(PTC)reaction of Ⅱ with 7 and the cyclization reaction of dicarbonyl acyclic precursor inducedby TiCl3-AlCl3(3:1)/Zn-Cu system.LI,Wei-Dong LI,Ying MAO,Jian-Min LI,Yu-Lin State Key Laboratory of Applied Organic Chemistry,Lanzhou University,Lanzhou 730000 1993Chinese Journal of Chemistry1993,11,2:1
8Transition-metal-free hydroamination/defluorination/cyclization of perfluoroalkyl alkynes with amidines显示文摘An efficient defluorinative net-[3+3]-cyclization strategy for the construction of perfluoroalkyl-substituted pyrimidine derivatives by using a series of perfluoroalkyl alkynes and amidines as starting materials was developed.The present reaction proceeded successfully under transition-metal-free conditions to form two new C–N bonds and a new heterocyclic ring through a sequence of hydroamination,defluorination,and annulation.The desired pyrimidines could be obtained with good functional group tolerance and moderate to good yields.Moreover,the distinctive fluorine effects of perfluoroalkyl substituents are vital for tuning the reactivity of alkynes for the anticipated defluorinative annulation.The pendantπsystem would lower associated bond dissociation energy significantly compared to that of a nonactivated C(sp^(3))–F bond.Li-Wen Sun Zi-Lun Yu Xin-Long Luo Mengtao Ma Zhi-Liang Shen Xue-Qiang Chu 2022Organic Chemistry Frontiers2022,9,1:1
9Sol-Gel Distribution of Polycondensation Reaction显示文摘A theoretical approach to polycondensation reaction of Aa-Bb type Involving intramolecular cycllzatlon has been proposed by Tang Au-chin et al.. In this paper, the theoretical sol-gel distribution is tested by polycondensation of adipic acid with trimethylol propane in a sto-ichiometric ratio of 0. 8, and the effect of intramolecular cyclization is discussed in detail.Li Zesheng, Ba Xlnwu, Sun Jiazhong and Tang Xinyi (Institute of Theoretical Chemistry and Department of Chemistry, Mm University, Changchun) 1990Chemical Research in Chinese Universities1990,6,4:1
10Enantioselective Synthesis of N-Phenyl-dihydropyrano[2,3-c]-pyrazoles via Cascade Michael Addition/Thorpe-Ziegler Type Cyclization Catalyzed by a Chiral Squaramide显示文摘Enantioselective synthesis of biologically active dihydropyrano[2,3-c]pyrazoles has been achieved through a squaramide-catalysed Michael addition/Thorpe-Ziegler type cyclization cascade reaction between arylidenepyra-zolones and malononitrile.A series of optically active dihydropyano[2,3-c]pyrazoles were obtained in excellent yields(up to 99%)and moderate to good enantioselectivities(up to 79%ee)under mild reaction conditions.Junhua Li Daming Du 2015Chinese Journal of Chemistry2015,33,4:1
11Development of aspartic acid ligation for peptide cyclization derived from serine/threonine ligation显示文摘Based on a mechanism analogous to the serine/threonine ligation, the aspartic acid ligation, which is facilitated by the γ-amino alcohol based ligation and oxidation, is developed and applied to the synthesis of cyclic peptides. The γ-hydroxyl group triggers the ring-chain tautomerization via a 6-endo-trig process,while the δ-hydroxyl group facilitates the oxidative cleavage of the vicinal diol to give carboxylic acid.Ci Xu Jianchao Xu Han Liu Xuechen Li 2018Chinese Chemical Letters2018,29,7:1
12Iron-Catalyzed Aminomethyloxygenative Cyclization of Hydroxy-α-diazoesters with N,O-Aminals显示文摘Summary of main observation and conclusion A new and eficient cyclization reaction has bleen developed to synthesize cyclic a,a-disubstituted B-amino esters via iron-catalyzed intramolecular aminomethyloxygenative cyclization of diazo compounds with N,O-aminal under mild reaction condi-tions.A broad range of hydroxy-a diazoesters with different substituents and various N,O-aminals were compatible with this protocol,affording the corresponding a,a-disubstitutedβ-amino esters bearing a five-to eight-membered oxacycle in good yields.Suchen Zou Tianze Zhang Siyuan Wang Hanmin Huang 2020Chinese Journal of Chemistry2020,38,4:1
13Rhodium(Ⅱ)-Catalyzed [4+3] Cyclization of Triazoles with Indole Derivatives and Its Application in the Total Synthesis of (±)-Aurantioclavine显示文摘An efficient rhodium(Ⅱ)-catalyzed[4+3]cyclization reaction of 1-sulfonyl-1,2-3-triazoles and indoles was developed.Azepino[5,4,3-ccflindoles,which are widely distributed in ergot alkaloids with various biological activities,could be obtained in good to excellent yields.In addition,the total synthesis of(±)-aurantioclavine was completed in four steps from the known compound 1a adopting this[4+3]cyclization as a key step.Shengguo Duan Bing Xue Hui Meng Zihang Ye Ze-Feng Xu Chuan-Ying Li 2021Chinese Journal of Chemistry2021,39,5:1
14Rh-Catalyzed Formal[3+2]Cyclization for the Synthesis of 5-Aryl-2-(quinolin-2-yl)oxazoles and Its Applications in Metal lons Probes显示文摘Main observation and conclusion A facile and efficient strategy for the synthesis of 5-aryl-2-(quinolin-2-yl)oxazoles via rhodium-catalyzed formal[3+2]cyclization of 4-aryl-1-tosyl-1H-1,2,3-triazoles with quinoline-2-carbaldehydes has been described.The protocol employs mild conditions and offers good yields of diverse 2,5-aryloxazole derivatives with a broad reaction scope.It is amenable to gram-scale synthesis and easily transformation.Moreover,this 5-aryl-2-(quinolin-2-yl)oxazole skeleton is indeed a new fluorophore and its applications in metal ions probes are also investigated and showed fluorescent responses to mercury ion.Tongtong Zhou Xinwei He Youpeng Zuo Yuhao Wu Wangcheng Hu Shiwen Zhang Jiahui Duan Yongjia Shang 2021Chinese Journal of Chemistry2021,39,3:1
15Total Synthesis of Starfish Cyclic Steroid Glycosides.Part 2,Model Synthesis via Intramolecular Etherification显示文摘Comprehensive Summary Sepositoside A(1)is a prototypical cyclic steroid glycoside bearing a hybrid 16-membered ring composed of the steroid skeleton and a 1,2-trans-linked trisaccharide.Herein,we report an expedient access toward two simplified analogues,in which the strained 16-membered ring is constructed via Au(I)-catalyzed intramolecular addition of alcohol to epoxide.A similar macroetherification in relevant steroid trisaccharides has been intensively examined,however,failed to furnish the macrocyclic skeleton of Sepositoside A.Youxi Chen Guozhi Xiao Dapeng Zhu Biao Yu 2023Chinese Journal of Chemistry2023,41,8:1
16One-Pot Synthesis of Spiro[fluorene-9,9'-xanthene]Derivatives显示文摘As a novel class of spirofluorenes,spirobifluorene(SBF)and spiro[fluo-rene-9,9'-xanthene]derivatives(SFXs)have orthogonal geometric config-uration,spiro-conjugation effect,and rigid steric hindrance,which can be widely used in the fields of synthetic chemistry,materials chemistry and supramolecular chemistry.Due to their facile one-pot synthetic route,and to the variety of molecular designs,SFXs are expected to become new spiro functional materials that replace SBF.In this review,we present the history,development and expansion of SFXs synthesis in one-pot methods,and the advantages and limitations of one-pot synthesis are also dis-cussed.Hao-Xuan Yuan Ying Wei Ling-Hai Xie Wei Huang 2021Chinese Journal of Chemistry2021,39,3:1
17Iron-Catalyzed Intramolecular C-H Amidation of N-Benzoyloxyureas显示文摘Main observation and conclusion A redox-neutral Fe-catalyzed intramolecular C-H amidation of N-benzoyloxyureas is described.This methodology employs a simple iron complex in situ generated from Fe(OTf)2 and bipyridine as the catalyst and N-benzoyloxyureas as the nitrene precursors without using exogenous oxidants.An array of cyclic ureas were synthesized via aliphatic C(sp^(3))-H amidation in excellent yields.In addition,this catalytic system is also amenable to aryl C(sp^(2))-H nitrene insertion to provide benzimidazolones in moderate yields.Dayou Zhong Lin-Yang Wu Xing-Zhen Wang Wen-Bo Liu 2021Chinese Journal of Chemistry2021,39,4:1
18Catalyst-free,direct electrochemical trifluoromethylation/cyclization of N-arylacrylamides using TfNHNHBoc as a CF_(3) source显示文摘A new electrochemical strategy for trifluoromethylation/cyclization using TfNHNHBoc as a CF_(3)source was established.This approach was realized by the direct electrolysis of Tf NHNHBoc under external oxidantfree and catalyst-free conditions,and afforded various trifluoromethylated oxindoles with good functional group compatibility and broad substrate scope.Preliminary mechanistic studies show that the reaction proceeds by a radical process.Han Wang Yongbin Xie Yicheng Zhou Nannan Cen Wenbo Chen 2022Chinese Chemical Letters2022,33,1:1
19Electrochemical Dearomative Halocyclization of Tryptamine and Tryptophol Derivatives显示文摘Summary of main observation and conclusion Owing to the easy functionalization of 3-haloindolines to many biologically active compounds,extensive efforts have been made for their efficient preparation.Herein,an electrochemical dearomative bromo-and chloro-cyclization of tryptamine and tryp-tophol derivatives has been developed under undivided electrolytic conditions.In this protocol,neither external chemical oxidants nor harsh conditions are needed,and a wide range of substituted hexahydropyrroloindolines/tetrahydrofuroindolines are obtained with halide ion in high efficiencies.Moreo-ver,this electrolysis could also be scaled up to gram synthesis with good yields.Kun Liu Yuqi Deng Wenxu Song Chunlan Song Aiwen Lei 2020Chinese Journal of Chemistry2020,38,10:1
20Synthesis of tetrahydroisoquinolines through TiCl4-mediated cyclization and Et3SiH reduction显示文摘A versatile and efficient telescoped reaction sequence for the synthesis of tetrahydroisoquinolines(THIQs)is reported that uses TiCl4 to promote cyclization of a benzylaminoacetal derivative and Et3SiH for reduction of the intermediate 4-hydroxy-THIQ.This method is complimentary to the classical Pomeranz-Fritsch and related reactions since it tolerates electron-withdrawing substituents and allows access to 8-substituted THIQs.Zeyu Shi Qiong Xiao Dali Yin 2020Chinese Chemical Letters2020,31,3:1
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