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Direct benzylic functionalization of pyridines:Palladium-catalyzed mono-α-arylation of α-(2-pyridinyl)acetates with heteroaryl halides 被引量:1
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作者 Chaochao Jin Kun Xu +2 位作者 Xiao Fan Changyao Liu Jiajing Tan 《Chinese Chemical Letters》 SCIE CAS CSCD 2020年第1期91-94,共4页
Herein,we report a Pd-catalyzed mono-a-arylation reaction for pyridine benzylic functionalization.This approach serves as an efficient alternative to synthesize di-heteroaryl acetates in good yields and selectivities.... Herein,we report a Pd-catalyzed mono-a-arylation reaction for pyridine benzylic functionalization.This approach serves as an efficient alternative to synthesize di-heteroaryl acetates in good yields and selectivities.Moreover,the method is applicable to heteroa ryl substrate combinations,and exhibits great functional group tolerance.A streamlined protocol also enables the rapid synthesis of diheteroaryl ketones.The synthetic value was also demonstrated by scale-up experiments. 展开更多
关键词 α-arylation Palladium HETEROCYCLES PYRIDINES Cross-coupling
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CuCl2/8-Hydroxyquinoline-catalyzed α-Arylation of Diethyl Malonate with Aryl Bromides
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作者 YANG Jiuquan WU Guojie +1 位作者 HE Yupeng HAN Fushe 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2018年第5期727-731,共5页
A general and efficient coupling of aryl bromides with diethyl malonate is presented. The reaction provided the α-arylated diethyl malonates in moderate to good yields with a low loading of CUC12(5%, molar fraction... A general and efficient coupling of aryl bromides with diethyl malonate is presented. The reaction provided the α-arylated diethyl malonates in moderate to good yields with a low loading of CUC12(5%, molar fraction) and 8-hydroxyquinoline(5% , molar fraction). This method has good compatibility for a wide range of aryl bromides. 展开更多
关键词 Copper catalyst α-arylation MALONATE Ullmann reaction Hurtley reaction
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studies on the Synthesis of Salvianolic Acid B. Synthesisof a 2-Aryl Dihydrobenzofuranoid Derivative
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作者 艾春波 黎莲娘 《Journal of Chinese Pharmaceutical Sciences》 CAS 1995年第3期161-164,共4页
报导了丹酚酸B结构中2-苯基二氢苯并呋喃部分甲基化衍生物的合成。
关键词 Salvianolic acid B 2-aryl dihydrobenzofuranoid Przewalskinic acid A
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Synthesis of 2-(N-formyl)-5-aryl/aryloxymethyl-1,3,4-thiadiazoles with potential bioactivity in PEG-400 被引量:1
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作者 Wang, Xi Cun Ding, Xiao Mei +2 位作者 Wang, Sheng Qing Chen, Xue Fei Quan, Zheng Jun 《Chinese Chemical Letters》 SCIE CAS CSCD 2010年第3期301-304,共4页
An environmental benign procedure for synthesis of 2-(N-formyl)-5-aryl/aryloxymethyl-1,3,4-thiadiazoles has been developed by reaction of 2-amino-5-aryl/aryloxymethyl-1,3,4-thiadiazoles with formic acid in PEG-400.The... An environmental benign procedure for synthesis of 2-(N-formyl)-5-aryl/aryloxymethyl-1,3,4-thiadiazoles has been developed by reaction of 2-amino-5-aryl/aryloxymethyl-1,3,4-thiadiazoles with formic acid in PEG-400.The key advantages of this protocol are the shorter reaction time,higher yields,lower cost,simple workup,and environment-friendly compared to conventional organic solvent reaction.The present method does not involve any hazardous organic solvent or catalyst. 展开更多
关键词 2-(N-Formyl)-5-aryl/aryloxymethyl-1 3 4-thiadiazoles 2-Amino-5-aryl/aryloxymethyl-1 PEG-400 Synthesis
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Synthesis,Characterization and Antibacterial Activity of New 5-Aryl Pyrazole Oxime Ester Derivatives
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作者 LIU Xin-hua ZHI Li-ping +1 位作者 SONG Bao-an XU Hong-li 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2008年第4期454-458,共5页
Eleven new 1-{5-[4-(benzyloxy)phenyl]-3-methyl-4,5-dihydropyrazol-l-yl} oxime ester dcrivatives were synthesized and characterized by elemental analysis, HRMS, ^1H NMR data. All the compounds were screened for their... Eleven new 1-{5-[4-(benzyloxy)phenyl]-3-methyl-4,5-dihydropyrazol-l-yl} oxime ester dcrivatives were synthesized and characterized by elemental analysis, HRMS, ^1H NMR data. All the compounds were screened for their antibacterial potential in vitro against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. The results indicate that compounds 8c and 8f possess potent activity with the minimum inhibitory concentrations(MIC) of 1.562--3.125 ug/mL against all the four bacteria. Compounds 8c, 8e and 8f show moderate inhibition against the DNA gyrase(IC50=1.9--2.5 ug/mL). On the basis of the biological activities, structure-activity relationship was discussed. 展开更多
关键词 5-aryl pyrazole Oxime ester Antibacterial activity
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Synthesis and Pregnancy Terminating Activity of 2-Aryl imidazo [2,1-a] isoquinolines
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作者 Gui Xiang HU Tian Xing WU +2 位作者 Zhi Cai SHANG Qing Sen YU Rui Ying FANG 《Chinese Chemical Letters》 SCIE CAS CSCD 2001年第6期499-500,共2页
Two 2-aryl imidazo [2,1-a] isoquinolines were synthesized and tested for pregnancy terminating activities. Both of them are new compounds and their structures were confirmed by IR, (HNMR)-H-1, MS and elemental analysi... Two 2-aryl imidazo [2,1-a] isoquinolines were synthesized and tested for pregnancy terminating activities. Both of them are new compounds and their structures were confirmed by IR, (HNMR)-H-1, MS and elemental analysis. They both showed high activities in NIH mice. 展开更多
关键词 2-aryl imidazo [2 1-a] isoquinolines SYNTHESIS pregnancy terminating activity
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Synthesis of 3-Aryl Coumarin Derivatives Using Ultrasound
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作者 Shubashini Krishnan Sripathi Kandasamy Logeeswari 《International Journal of Organic Chemistry》 2013年第1期42-47,共6页
Coumarins occupy an important place in the realm of natural products and synthetic organic chemistry. A fast and highly efficient green method for synthesizing 3-aryl coumarin derivatives from salicylaldehyde and phen... Coumarins occupy an important place in the realm of natural products and synthetic organic chemistry. A fast and highly efficient green method for synthesizing 3-aryl coumarin derivatives from salicylaldehyde and phenyl acetyl chloride in the presence of tetrahydrofuran and K2CO3 using ultrasound irradiation is reported. Ultrasound assisted reactions have resulted in better yields and faster reaction time of the desired products than when prepared under conventional conditions. The resulting coumarin derivatives were characterized by IR spectrum. 展开更多
关键词 3-aryl COUMARIN TETRAHYDROFURAN K2CO3 SALICYLALDEHYDE Phenyl Acetyl Chloride ULTRASOUND
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Free amino group-directed C(sp^(2))-H arylation ofα-amino-β-aryl esters by palladium catalysis
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作者 Yue Gao Yu Du Weiping Su 《Chinese Chemical Letters》 SCIE CAS CSCD 2024年第2期358-360,共3页
Native amino-directed palladium-catalyzed C(sp^(3))-H activation/functionalization has been developed for modification ofα-amino acids and peptides.Herein a palladium(Ⅱ)-catalyzed C(sp^(2))-H arylation ofα-amino-β... Native amino-directed palladium-catalyzed C(sp^(3))-H activation/functionalization has been developed for modification ofα-amino acids and peptides.Herein a palladium(Ⅱ)-catalyzed C(sp^(2))-H arylation ofα-amino-β-aryl esters has been disclosed,using the native amino as the directing group.A variety of chiralα-amino-β-aryl esters can be functionalized to give the corresponding ortho-substituted mono-and di-arylated products. 展开更多
关键词 Native amino-directed Palladium catalyst C(sp^(2))-H arylation α-Amino-β-aryl ester Chiralα-amino acid
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Studies on the Synthesis, Anticonvulsant Activity, and the Structure-Activity Relationships of Phenyl Pyridazinones and their GABA Derivatives
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作者 徐萍 王书玉 刘维勤 《Journal of Chinese Pharmaceutical Sciences》 CAS 1992年第2期27-34,共8页
In searching for effective anticonvulsant agents,fourteen 6-aryl-4.5-di- hydro-3(2H)pyridazinones.fifteen 6-aryl-3(2H)pyridazinones,and seventeen 3-GABA derivatives of 6-aryIpyridazines have been synthesized,and evalu... In searching for effective anticonvulsant agents,fourteen 6-aryl-4.5-di- hydro-3(2H)pyridazinones.fifteen 6-aryl-3(2H)pyridazinones,and seventeen 3-GABA derivatives of 6-aryIpyridazines have been synthesized,and evaluated in mice for the ability to antagonize maximal electroshock seizure(MES).The ED_(50) values showed that 6-(2′,4′- dichlorophenyt)-3(2H)pyridazinone was the most potent anticonvulsant among these corn- pounds(ED_(50)=10.15 mg/kg).The structure-activity relationships of the aryl pyridazinones were studied.The result showed that:(1)the higher the value of the hydrophobic parameter л of the substituent on the phenyl ring.the more potent the anticonvulsant activity of the corn- pound.and(2)only the compounds with an electron withdrawing substituent on the phenyl ring exhibited appreciable anticonvulsant activity. 展开更多
关键词 Aryl pyridazinones 3-GABA-6-aryl pyridazines Anticonvulsant activity Structure-activity relationships
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A new approach to the bicyclo[3.3.1]nonane framework of huperzine A-like molecules via palladium-catalyzed intramolecular γ-arylation 被引量:2
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作者 DING Rui LU YunYu +2 位作者 YAO HeQuan SUN BingFeng LIN GuoQiang 《Science China Chemistry》 SCIE EI CAS 2012年第6期1097-1100,共4页
In our synthetic studies toward huperzine A, a diastereoselective α'-alkylation of the α-amido-γ-methyl hexenone 4 was real- ized through a dianion intermediate which significantly enhanced the reactivity. Under t... In our synthetic studies toward huperzine A, a diastereoselective α'-alkylation of the α-amido-γ-methyl hexenone 4 was real- ized through a dianion intermediate which significantly enhanced the reactivity. Under the attempted Heck reaction conditions, an unexpected and unprecedented palladium-catalyzed intramolecular T-arylation of 3 was observed, which generated 18 with bicyclo[3.3, l]nonane framework in satisfactory yield. 展开更多
关键词 huperzine A bicyclo[3.3.1]nonane γ-arylation
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Kinetic Resolution of Racemic 4-Substituted Chroman-2-ones Through Asymmetric Lactone Hydrogenation
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作者 Xiong Wu Hai-Tao Yue +4 位作者 Xiao-Dong Zuo Xiao-Hui Yang Pu-Cha Yan Jian-Hua Xie Qi-Lin Zhou 《CCS Chemistry》 CSCD 2024年第10期2560-2576,共17页
Esters are abundant in natural and synthetic products and their conversion into primary alcohols holds great importance in fine chemical synthesis.However,achieving asymmetric hydrogenation(AH)of racemic esters with r... Esters are abundant in natural and synthetic products and their conversion into primary alcohols holds great importance in fine chemical synthesis.However,achieving asymmetric hydrogenation(AH)of racemic esters with remote stereocenters via kinetic resolution(KR)remains a formidable challenge due to the difficulties associated with discerning spatially distant stereocenters.To address this issue,we have designed a hydroxy-assisted strategy that introduces a hydroxy group into racemicβ-aryl esters to facilitate hydrogenation and enhance chiral discrimination through a lactone form.By employing chiral Ir-SpiroPAP catalysts,we achieved exceptional AH of racemic 4-substituted chroman-2-ones,lactone form of ortho-hydroxylatedβ-aryl esters,via KR,resulting in impressive selectivity factor(s)values of up to 600.This approach exhibited significant efficacy for racemic chroman-2-ones containingβ-aryl,alkenyl,alkynyl,and alkyl groups,enabling the synthesis of chiralγ-aryl primary alcohols and the recovery of chiralβ-aryl esters or chroman-2-ones,typically difficult to access using existing methods.The scalability and broad synthetic applications of this method were exemplified by successfully synthesizing chiral drugs(R)-fesoterodine and enrasentan,alongside various chiral intermediates essential for producing chiral drugs and natural products.These promising results highlight the potential of this approach as a powerful tool for synthesizing valuable chiral compounds. 展开更多
关键词 asymmetric hydrogenation chiralγ-aryl primary alcohols hydrogenation of esters iridium catalysts kinetic resolution
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Visible-Light-Induced Cascade Azidation/Cyclization of Activated Alkenes to Synthesize Azidated Indolo[2,1-a]isoquinolines
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作者 Tang Yucai He Yupeng +7 位作者 Yang Biyu Duan Jinglin Du Changyuan Jiang Jie Li Jiali Pan Ruohan Chen Yu Liu Xuewen 《有机化学》 SCIE CAS CSCD 北大核心 2024年第7期2286-2295,共10页
An efficient visible-light-induced radical cascade azidation/cyclization of 2-aryl indoles with trimethylsilyl azide(TMSN3)has been developed using organic dye Rose Bengal as the photocatalyst.This method did not requ... An efficient visible-light-induced radical cascade azidation/cyclization of 2-aryl indoles with trimethylsilyl azide(TMSN3)has been developed using organic dye Rose Bengal as the photocatalyst.This method did not require metal catalysts and additives,and used air as the oxidant to obtain diverse indolo[2,1-a]isoquinolin-6(5H)-ones in moderate to good yields.Mechanistic studies demonstrated that the reaction proceeded via a radical pathway. 展开更多
关键词 Rose Bengal visible-light 2-aryl indole AZIDATION indolo[2 1-a]isoquinolin-6(5H)-one
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Synthesis of Novel 3-Aryl Isoindolinone Derivatives 被引量:2
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作者 HU Chen-ming ZHENG Lian-you PEI Ya-zhong BAI Xu 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2013年第3期487-494,共8页
A library of novel 3-aryl isoindolinone derivatives with aromatic amino acid derivative fragments was designed and synthesized. Two synthetic routes were employed to construct 3-aryl isoindolinone ring system for diff... A library of novel 3-aryl isoindolinone derivatives with aromatic amino acid derivative fragments was designed and synthesized. Two synthetic routes were employed to construct 3-aryl isoindolinone ring system for different amino acid derivatives. 展开更多
关键词 Molecular library 3-aryl isoindolinone Aromatic amino acid derivative
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Synthesis of 14-aryl or alkyl-14H-dibenzo[a,j]xanthenes promoted by Mg(HSO_4)_2 被引量:1
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作者 Bi Bi Fatemeh Mirjalili Abdolhamid Bamoniri Ali Akbari 《Chinese Chemical Letters》 SCIE CAS CSCD 2011年第1期45-48,共4页
14-Aryl or alkyl-14H-dibenzo[a,j]xanthenes were prepared by condensation of 2-naphthol and aldehydes in the presence of Mg(HSO4)2 as an efficient, cheap, readily available and eco-friendly catalyst. This procedure h... 14-Aryl or alkyl-14H-dibenzo[a,j]xanthenes were prepared by condensation of 2-naphthol and aldehydes in the presence of Mg(HSO4)2 as an efficient, cheap, readily available and eco-friendly catalyst. This procedure has the advantages of high yields, easy work-up, short reaction times, and green conditions. 展开更多
关键词 14-aryl or alkyl-14H-dibenzo [a j]xanthene Mg(HSO4)2 XANTHENES 2-Naphthol Ultrasound
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Preparation of 2-amino-5,7-dimethoxy-4-aryl/alkyl-4H-chromene-3-carbonitriles using Na_2O-Al_2O_3-P_2O_5 glass–ceramic system 被引量:1
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作者 Saeid Jabbarzare Majid Ghashang 《Chinese Chemical Letters》 SCIE CAS CSCD 2015年第11期1385-1388,共4页
A highly efficient and environmentally benign protocol for the synthesis of 2-amino-5,7-dimethoxy-4- aryl/alkyl-4H-chromene-3-carbonitrile derivatives by one-pot three-component coupling reacting of aromatic aldehydes... A highly efficient and environmentally benign protocol for the synthesis of 2-amino-5,7-dimethoxy-4- aryl/alkyl-4H-chromene-3-carbonitrile derivatives by one-pot three-component coupling reacting of aromatic aldehydes, malononitrile and 3,5-dimethoxy phenol under reflux condition has been developed in aqueous EtOH media using Na2O-Al2O3-P2O5 glass-ceramic system. 展开更多
关键词 Na2O-Al2O3-P2O5 glass-ceramic system2-Amino-4H-chromene3 5-Dimethoxy phenol2-Amino- 5 7-dimethoxy-4-aryl/alkyl-4H-chromene-3-carbonitriles
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A NEW SYNTHETIC ROUTE TO α-ARYL PROPIONIC ACID AND A QUANTITA-TIVE STUDY OF THE PHOTO-S_(RN)1 REAC-TION OF ARYL HALIDES WITH CAN-BANION FROM ALKYL NITRILE
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作者 吴碧琪 曾繁文 +2 位作者 葛明娟 程新中 吴国生 《Science China Chemistry》 SCIE EI CAS 1991年第7期777-786,共10页
A new synthetic route leading to α-(2-(6-methoxynaphthy1))-propionic acid has ben developed. Successive one-step preparation of the appropriate α-aryl propionitrile from the aryl halides with propionitrile by photo-... A new synthetic route leading to α-(2-(6-methoxynaphthy1))-propionic acid has ben developed. Successive one-step preparation of the appropriate α-aryl propionitrile from the aryl halides with propionitrile by photo-SRN1 procedure followed by hydrolysis gives the desired α-aryl propionic acid in excellent total yield. The photostimulated reaction of 2-bromonaph-thalene with acetonitrile or propionitrile in KNH2-NH3 solution to form the corresponding nucleophilic substitution product occurs with quantum yields considerably in excess of unit, while the pseudo-first-order rate constants of the photo-SRN1 are 30.9 and 47.0×10-5mol·s-1, respectively. Definite evidence to support the excitation of ground CTC and electron transfer from anion to ArX within the complex comes from the observation of the same φ>200 and φ>313 as well as MO calculation. 展开更多
关键词 α-aryl propionie ACID group CTC MO calculation.
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Synthesis of 1-acyl-5-aryl biurets
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作者 ZOU, JP LU, ZE CHEN, KQ 《Chinese Journal of Chemistry》 SCIE CAS CSCD 1995年第4期358-362,共5页
Fourteen new 1-acyl-5-aryl biurets were synthesized by the reaction of aryl ureas with acylisocynantes. The latter was obtained from acyl. chloride and lead cyanate in dichloromethane, using pyridine as catalyst. The ... Fourteen new 1-acyl-5-aryl biurets were synthesized by the reaction of aryl ureas with acylisocynantes. The latter was obtained from acyl. chloride and lead cyanate in dichloromethane, using pyridine as catalyst. The structures of compounds 3a-n were confirmed by IR, H-1 NMR and MS spectra. 展开更多
关键词 1-ACYL-5-aryl BIURET ACYLISOCYANATE ARYLUREA SYNTHESIS
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A convenient catalytic oxidative 1,2-shift of arylalkenes for preparation of α-aryl ketones mediated by NaI
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作者 Min Zhu Yang Zhao 《Chinese Chemical Letters》 SCIE CAS CSCD 2015年第2期248-250,共3页
Using a catalytic amount of Nal and a stoichiometric oxidant Oxone-@,a convenient procedure has been developed for the catalytic oxidative 1,2-shift of arylalkenes in CH3CN/H2O at room temperature,which provides the c... Using a catalytic amount of Nal and a stoichiometric oxidant Oxone-@,a convenient procedure has been developed for the catalytic oxidative 1,2-shift of arylalkenes in CH3CN/H2O at room temperature,which provides the corresponding α-aryl ketones in moderate to good yields.In this protocol,sodium iodide is first oxidized into hypoiodous acid,which reacts with arylalkene to afford iodohydrin.Then,the iodohydrin is transformed into the α-aryl ketone via an oxidative 1,2-shift rearrangement. 展开更多
关键词 Oxidative 1 2-shift α-aryl ketone Sodium iodide Catalysis
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Iodine Catalyzed Microwave-Assisted Synthesis of 14-Aryl(Alkyl)-14H-dibenzo[a,j]xanthenes
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作者 丁飞青 安礼涛 邹建平 《Chinese Journal of Chemistry》 SCIE CAS CSCD 2007年第5期645-648,共4页
A straightforward and effective procedure for the synthesis of 14-aryl(alkyl)-14H-dibenzo[aj]xanthenes was described using a catalytic amount of molecular iodine under microwave irradiation to afford the correspondi... A straightforward and effective procedure for the synthesis of 14-aryl(alkyl)-14H-dibenzo[aj]xanthenes was described using a catalytic amount of molecular iodine under microwave irradiation to afford the corresponding xanthenes in good yields. 展开更多
关键词 14-aryl(alkyl)-14H-dibenzo[a.j]xanthene microwave irradiation molecular iodine
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Design, Synthesis and Pregnancy-Terminating Activity of 2-Aryl Imidazo[2,1-a]isoquinolines
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作者 商志才 胡桂香 +2 位作者 吴天星 方瑞英 俞庆森 《Chinese Journal of Chemistry》 SCIE CAS CSCD 2004年第3期315-320,共6页
In order to clarify the structural requirement of pregnancy-terminating drugs, the quantitative structure-activity relationship (QSAR) of 2-aryl imidazo[2,1-a]isoquinolines was studied on the basis of quantum mechanic... In order to clarify the structural requirement of pregnancy-terminating drugs, the quantitative structure-activity relationship (QSAR) of 2-aryl imidazo[2,1-a]isoquinolines was studied on the basis of quantum mechanical calculation and multiple regression analysis. A Good correlation equation was obtained (r2=0.925, q2=0.871). Some new compounds were designed according to the equation. Two of them, compounds 21 and 22, were synthesized and evaluated in NIH mice. The results showed that the difference of activity between 21 (median effective dose ED50=0.943 mg/kg/day) and 22 (ED50=1.099 mg/kg/day) was small and both of them were potent. It is also agreed with the computational results. Compared with L14105 which is the most potent pregnancy-terminating agent, these two compounds possess high activity. The evaluation of the anti-implanting activity showed that they were 100% effective at tested dosage 50.0, 25.0, 12.5 mg/kg/day×3 days in oral administration, which proved the both of them had anti-implanting activity and low first-pass effects. 展开更多
关键词 2-aryl imidazo[2 1-a]isoquinolines quantitative structure-activity relationship (QSAR) pregnancy- terminating activity anti-implanting first-pass effect
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