顺-1-环已基-3-酰氨基-4-取代苯基-2-氮杂环丁酮的合成

近年来单环β-内酰胺类抗生素的研宄引起了人们的极大兴趣。β-内酰胺类抗生素广泛使用所导致的病原菌的耐药性日趋严重,迫切需要寻找新的抗生素和β-内酰胺酶抑制     

Synthesis of Diaryl Ethers, Diaryl Sulfides, Heteroaryl Ethers and Heteroaryl Sulfides under Microwave Heating

Diaryl ether moiety is found in a pool of naturally occurring and medicinally important compounds.[1] As a consequent, considerable efforts have been devoted to the assembly of this framework.[2] Recently, we have developed a microwave heating version of the synthesis of diaryl ethers as well as aryl sulfides. Under our conditions, even the extremely electron-poor 4-nitrophenol works well and its reaction with 1-halo-4-nitrobenzenes produces 4-(nitrophenoxy)-benzonitriles in satisfactory yield. The scope of the present protocol has been expanded to hydroxylated six-membered heterocycles as well as 2-pyrimidinethiol with mildly activated aryl halides, affording heteroaryl ethers and respectively sulfides. The advantages of the present method include the wide substrate scope, no use of any metal catalysts, the ease of product isolation and high yields.     

Design,Synthesis and Antimicrobial Evaluation of Novel Tricyclic Benzoxazine Fluoroquinolones under Conventional and Microwave Methods

In view of obtaining some potential antimicrobial compounds, we have described synthesis of novel fluoroquinolones bearing 2‐(piperidin‐4‐yl)‐1H‐benzo[d]imidazole and evaluated for their antimicrobial activity. Alternatively, synthesis of these products was also demonstrated using microwave irradiation technique. The antimicrobial activity of newly synthesized compounds was evaluated against number of microorganisms and the activity is compared with highly active levofloxacin.     

Synthesis and Solid State Fluorescence of Malononitrile Trimer Ylidene Derivatives in Aqueous Medium under Ultrasonication

Russian Journal of Organic Chemistry - Potassium salts of benzylidene and cinnamylidene derivatives of malononitrile trimer were obtained by reactions of substituted benzaldehydes and...     

Thiazolidinones: Synthesis,Reactivity, and Their Biological Applications

Thiazolidinone is a biologically important five‐membered heterocyclic ring having almost all types of biological activities. This review covers various types of thiazolidinones, such as 2‐thiazolidinones, 4‐thiazolidinones, 5‐thiazolidinones, 2‐thioxo‐4‐thiazolidinones, and thiazolidiene‐2,4‐dione. The literature related to the physical properties, chemical reactions, and synthesis for these derivatives has been included. Recent advances in the biological activities reported for 4‐thiazolidinone derivatives, such as peroxisome proliferator‐activated receptor γ binders, follicle‐stimulating hormone agonists, cystic fibrosis transmembrane conductance regulator inhibitors, and antioxidants, have been covered in this review. Thus, this study may help in further optimizing these thiazolidinone derivatives as more effective drug agents.     

超声条件下制备单取代硼酸

本文报道以硼酸三丁酯为原料与卤代烃,金属镁粉在室温下经超声辐射制备单取代硼酸的结果。该方法操作简单,反应速度快,并得到满意的产率,有一定的应用价值。     

Synthesis and Biological Activity of Mercaptobenzoxazole Based Thiazolidinones and Their Arylidenes

Arylidenes of thiazolidines with mercaptobenzoxazole, namely[(aryl‐4‐oxo‐1,3‐thiazolidin)‐hydrazinoacetyl‐mercaptobenxazole]; (5‐arylidene)‐2‐aryl‐4‐oxo‐1,3‐thiazoliden hydrazinoacetyl‐mercaptobenxazole were synthesized. Their chemical structures have been confirmed by ¹H NMR, IR, mass spectra and also by microanalytical data. Antimicrobial evaluation was done by agar dilution method against three pathogenic bacteria viz. Bacillus subtilis, Escherichia coli and Klebsiella pneumoniae and three pathogenic fungi viz. Aspergillus niger, Candida albicans and Fusarium oxysporum. Among new derivatives evaluated, the chloro derivatives exhibited higher potency as compared to the standard drugs streptomycin (for bacteria) and griseofulvin (for fungi) against the tested organisms.     

一锅法合成芳(杂环)胺亚甲基双膦酸四乙酯

以I₂为催化剂,原甲酸三乙酯、芳(杂环)胺和亚磷酸二乙酯为原料,室温无溶剂条件下,一锅合成了系列芳(杂环)胺亚甲基双膦酸四乙酯,收率96%~99%。 当I₂物质的量分数为5%时,产物收率最高。 本方法底物适用范围广,操作简单。 I₂作为催化剂,安全高效。     

Synthesis of Some New 2,4-Disubstituted Hydrazinothiazoles and 2,5-Disubstituted Thiazolidinones

A series of hydrazinothiazoles has been synthesized by the condensation of thiosemicarbazones and α-bromoketones. Similarly the hydrazinothiazolidiones were prepared by the condensation of thiosemicarbazone and α-bromoesters. The newly synthesized compounds were characterized by NMR and LCMS studies.     

单苯并15-冠-5的超声作用合成

以邻苯二酚、一缩二乙二醇双氯乙醚为原料,氢氧化钠为模板剂,DMF为溶剂及适量抗氧化剂2,6-二-叔丁基对甲苯酚存在下,在超声辐射作用下60~70 ℃反应合成了B-15-C-5。 反应时间缩短为2 h,产率最高可达30.7%。     

Chemoselective Synthesis of Polysubstituted Pyridines from Heteroaryl Fluorosulfates

A selection of heteroaryl fluorosulfates were readily synthesized using commercial SO₂F₂ gas. These substrates are highly efficient coupling partners in the Suzuki reaction. Through judicious selection of Pd catalysts the fluorosulfate functionality is differentiated from bromide and chloride; the order of reactivity being: ‐Br> ‐OSO₂F> ‐Cl. Exploiting this trend allowed the stepwise chemoselective synthesis of a number of polysubstituted pyridines, including the drug Etoricoxib.     

Synthesis and Antitubercular activity of New Thiazolidinones with Pyrazinyl and Thiazolyl Scaffolds

Emergence of multidrug resistant and extensively drug resistant tuberculosis has prompted to develop new molecular entities to treat the disease. A series of new 4‐thiazolidinones with pyrazinyl and thiazolyl scaffolds has been synthesized, and their antitubercular activity is reported. The title 4‐thiazolidinones, N‐(pyrazinyl substituted thiazoloylamino)‐2‐aryl‐4‐thiazolidinones ( 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h , 6i , 6j ) have been first time prepared using pyrazinamide as a starting material via five successive steps. The purity and the structures of the intermediates (carboethoxythiazole, acid hydrazide, and azomethines) and title thiazolidinones ( 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h , 6i , 6j ) have been confirmed by TLC and spectral analyses, respectively. An antitubercular screening of the new 4‐thiazolidinones has been performed on bacterial strains, Mycobacterium tuberculosis H37Ra and Mycobacterium BCG using the solutions of different concentrations of the compounds ( 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h , 6i , 6j ) and the screening results are presented. Compound 6a has displayed notable antitubercular activity.     

Synthesis of Benzazolyl Pyrimidines Under Ultrasonication and Their Antimicrobial Activity

(1) The benzoxazolyl/benzothiazolyl/benzimidazolyl pyrimidines were prepared under ultrasonication in the presence of pyridine/dimethylaminopyridine and triethylamine. (2) Better yields were recorded in 4‐(N,N‐dimethylamino)pyridine and Et₃N. (3) The presence of electron withdrawing chloro, bromo, and nitro substituents enhanced antimicrobial activity ( 13c , 13e , 14e : minimum inhibitory concentration = 6.25 μg/well against Bacillus subtilis; 13e , 14e : minimum inhibitory concentration = 6.25 μg/well against Aspergillus niger).     

Parallel Synthesis and Testing of Catalysts under Nearly Conventional Testing Conditions

Acceleration by one to two orders of magnitude for catalyst development without much loss of information: Parallelized synthesis and screening has been used to evaluate catalysts for the room-temperature oxidation of CO. The overall process was highly reproducible, and the data quality is comparable to that of conventional testing. The graph shows the results of parallel testing of Au/Co₃O₄ catalyts at 25°C (y=yield of CO₂).     

Synthesis of 1,2-Disubstituted Ferrocene Containing a Heteroaryl Group

A convenient synthesis of [C₅H₅Fe(1,2-C₅H₃(CH₂R)(Heteroaryl)], (R=NMe₂, Heteroaryl=5-benzoylthien-2-yl(3a), 2-nitropyrid-5-yl(3b), 5-nitrothien-2-yl(3c), 6-methoxy-8-nitroquino-3-yl(3d); R=MeO, Heteroaryl=5-benzoylthien-2-yl(6a), 2-nitropyrid-5-yl)(6b) from [C₅H₅Fe(1,2-C₅H₃(CH₂R)(SnBu₃)], (R=NMe₂, OMe), via Stille coupling reaction is described.     

Synthesis of Five-Membered Ring Heteroaryl Pyridines from Heteroaryllithium and N-Ethoxycarbonylpyridinium Chlorides

Furylpyridines, thienylpyridines, and imidazolylpyridines were obtained regioselectively in 40-67% yields from the reaction of heteroaryllithiums with N-ethoxycarbonylpyridinium chloride or N-ethoxycarbonyl-3-methylpyridinium chloride in the presence of Cul in a catalytic amount at ?78 °C or ?50°C, then followed by oxidation. The regioselectivity of this reaction depended upon temperature of the reaction and the nature of heteroaryllithiurn.     

Synthesis of Ionic Liquids Using Non Conventional Activation Methods: An Overview

Summary. The synthesis of ionic liquids under non conventional activation methods is historically reviewed and completed with the recent developments of “one-pot” synthesis and combination of these activation methods.     

An Improved Synthesis of 1,2-Diarylethanols under Conventional Heating and Ultrasound Irradiation

A simple and efficient synthesis of 1,2-diarylethanols has been developed. The procedure involved the reaction between a variety of toluene derivatives and aryl aldehydes under conventional heating and ultrasound irradiation. This procedure possesses several advantages such as operational simplicity, high yield, safety and environment benignancy. Ultrasound was proved to be very helpful to the reaction, markedly improving the yield and the reaction rate.     

Synthesis of Ionic Liquids Using Non Conventional Activation Methods: An Overview

The synthesis of ionic liquids under non conventional activation methods is historically reviewed and completed with the recent developments of “one-pot” synthesis and combination of these activation methods.