A Facile Synthesis of 3,5—Diaryl 1,2,4—Selenadiazoles from Aryl Selenoamides

A facile synthesis of 3,5-diaryl 1,2,4-selenadiazoles was provided by treatment of aryl selenoamides with p-methylphenyl sulfonyl chloride in chloroform.     

Synthesis of 4—Aryl—3,4—dihydropyrimidinones Using Microwaveassisted Solventless Biginelli Reaction

Ｉｎｔｒｏｄｕｃｔｉｏｎ4 Ａｒｙｌ 3,4 ｄｉｈｙｄｒｏｐｙｒｉｍｉｄｉｎｏｎｅｓ (4)ａｓａｃｏｒｅｗｅｒｅｏｂｓｅｒｖｅｄｉｎｓｏｍｅｂｉｏｌｏｇｉｃａｌｌｙｉｍｐｏｒｔａｎｔｃｏｍｐｏｕｎｄｓ .1Ｍｏｒｅｒｅｃｅｎｔｌｙ ,ｄｉｈｙｄｒｏｐｙｒｉｍｉｄｉｎｏｎｅｓａｒｅｓｈｏｗｎｔｏｂｅａｕｓｅｆｕｌｔｏｏｌｆｏｒｓｔｕｄｙｉｎｇｄｙｎａｍｉｃｃｅｌｌｕｌａｒｐｒｏｃｅｓｓａｎｄｃａｎｂｅｃｏｎｓｉｄｅｒｅｄａｓａｎｅｗｌｅａｄｆｏｒｔｈｅｄｅｖｅｌｏｐｍｅｎｔｏｆａｎｔｉ ｃａｎｃｅｒｄｒｕｇ…     

Synthesis and Biological Activities of 3—（2—Furyl）—4—aryl—1,2,4—triazole—5—thiones

A series of novel compounds 3-(2-furyl)-4-aryl-1,2,4-triazole-5-thiones have been synthesized.All the compounds were characterized by spectral data and elemental analysis. The preliminary biological test showed that some of them exhibited excellent plant-growth regulative activities.     

CuI-catalyzed Synthesis of Aryl Thiocyanates from Aryl Iodides

Aryl thiocyanates are important compounds not only for their interesting biological properties, but also because of their use as a versatile starting material for many sulfur- containing aromatic compounds, including sulfonyl cyanides, sulfonic acids, sul…     

Synthesis of 5—Deoxy—5—Acyloxyiminoavermection B1 Derivatives

Four 5-deoxy-5-acyloxyiminoavermectin B1 derivatives 4a-d were synthesized via three steps from avermenction B1 and their biological activities were tested against Heliothis armigera, Laphygma exigua and Musca domestica.     

A New Solution—phase Parallel Synthesis of 2—Alkyamino—3—aryl—5—phenylmethylene—3,5—dihydro—4H—imidazol—4—ones

Thirteen new 2-alkylaminoimidazolones(4) wre rapidly synthesized by a new solution-phase parallel synthetic method,which includes aza-Wittig reaction of iminophosphorane(1) with aromatic isocyanate to give carbodi-imide(2) and subsequent reaction of 2 with various aliphatic primary amine in a parallel fashion.The products were confirmed by ^1H NMR,MS,IR and X-ray crystallographic analysis.The unusual selectivity of the cyclization was probably due to the deometry of the guanidine intermediate.     

Synthesis of 3—Biaryl—1—ferrocenyl—2—propene—1—ones

The novel structures of organometallic compounds 3-biaryl-1-ferrocenyl-2-propene-1-ones 5 were synthesized for nonlinear optical chromophores by Suzuki cross-coupling reaction.Their structures were determined with elemental analyses,^1H NMR spectra and ^13C NMR spectra.     

Synthesis and Biological Activities of 4-Arylmethylidene-1-aryl-2-（selenomorpholin-4-yl） -2-imidazolin-5-one

In a search for novel agrochemical with high activity and low toxicity, a series of substituted 4,5-dihydro-imidazol-5-one containing selenomorpholine group were synthesized by a three-step synthetic route starting from 2-azido-3-aryl-acrylic acid ethyl ester. The structures of title compounds were confirmed by ^1H NMR, IR, mass spectroscopy and elemental analysis. The preliminary bioassay against GibbereUa zeae, Fusarium oxysporum, Pellicularia sasakii, Physalospora piricola and Cercospora beticola indicated that most title compounds displayed fungicidal activity at the concentration of 50 ppm and compounds 41,4n, 40 were found to have particularly high activities against Physalospora piricola. A further in vivo test showed that compounds 41, 4n and 4o possessed better fungicidal activity against Physalospora piricola at a concentration of 100 ppm than Carbendazim. To our knowledge, this is first report that 4,5-dihy-dro-imidazol-5-one containing selenomorpholine group display fungicidal activity against Physalospora piricola.     

Synthesis of （1H）—3,4—Dithydropyrrolo[2,1—c][1,4]oxazin—1—one Derivatives

In search of new anti-inflammatory and analgesic agents,(1H)-3,4-dihydro-pyrrolo [2,1-c][1,4]oxazin-1-one(3) and its acyl derivatives were designed and prepared .Compound 3 was prepared by treatment of methyl 1-(2-bromoethyl) pyrrole-2-carboxylate with silver oxide and its derivatives were obtained by Friedel-Carftes reaction.Nine of 6-acyl derivatives of compound 3 were prepared.     

Synthesis and Antibacterial Activities of 4—Amino—3—（1—aryl—5—methyl—1,2,3—triazol—4—yl）—5—mercapto—1,2,4—triazoles／2—Amino—5—（1—aryl—5—methyl—1,2,3—triazol—4—yl）—1,3,4—

Treatment of 4-amino-3-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-5-mercapto-1,2,4-triazoles/2-amino-5-(1-aryl-5-methyl-1,2,3-triazole-4-yl)-1,3,4-thiadiazoles with benzaldehyde,acetone and ω-bromoacetophenone was tested and compared.The title compounds Schiff bases,amides,imidazolo [2,1-b]-1,3,4-thiadiazoles and 7H-s-triazolo[3,4-b]-1,3,4-thiadiazines have been confirmed by elemental analyses,^1H NMR,IR and MS spectra.All the compounds have also been screened for their antibacterial activities against B.subtilis,S.aureus and E.coli.     

Synthesis of 1-aryl-3-（3,4-dihydro-2H-chromen-5-yl） ureas as TNF-α inhibitors

A new series of compounds,1-aryl-3-(3,4-dihydro-2H-chromen-5-yl) ureas,have been synthesized and their structures were confirmed by FAB-MS and ~1H NMR.The preliminary pharmacological screening showed that these compounds inhibited TNF-αproduction in lipopolysaccharide (LPS)-stimulated THP-1 cells.     

Facile Iodine(III)-Mediated Approach for the Regioselective Chlorination of 2-Aryl-2,3-dihydro-4(1H)-quinolones

Oxidation of 2-aryl-2,3-dihydro-4(1H)-quinolones (1) with 1.5 equivalents of (dichloroiodo)benzene in dichloromethane at room temperature leads to regioselective chlorination, thereby offering an efficient method for the synthesis of new 2-aryl-6-chloro-2,3-dihydro-4(1H)-quinolones (3).     

The Synthesis of 1-Aryl-5-Fluorouracil

5-Fluorouracil (5-Fu,1)1 is an important antitumor drug. Some derivatives2,3 have shown better therapeutic efficacy than 5-Fu. In order to find much more better antitumor drugs of its derivatives, several attempts have been made and many different types of its derivatives have been prepared at N1, N3 position4~7. Moreover, several different ways have been used for alkylation of 5-Fu7~10. However, up to now, the arylation of 5-Fu at N1 or N3 position hasn't been reported, and the compound o…     

Synthesis of 5-[2-(Phenoxy)ethyl] Derivatives of 6-Methyluracil, 6-Methyl-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one,and 2-Imino-6-methyl-2,3-dihydro-1H-pyrimidin-4-one

A synthesis of novel derivatives of 6-methyluracil, 6-methyl-2-thioxo-, and 2-imino-6-methyl-2,3-dihydro-1H-pyrimidin-4-one containing a 2-(phenoxy)ethyl substituent at position 5 of the pyrimidine ring has been carried out. It was found that 5-[2-(phenoxy)ethyl] derivatives of 6-methyl-2-thioxo- and 2-imino-6-methyl-2,3-dihydro-1H-pyrimidin-4-one are obtained by the condensation of the corresponding ethyl 3-oxo-2-(2-phenoxyethyl)butanoates with thiourea or guanidine. 6-Methyl-5-[2-(phenoxy)ethyl]uracils can be prepared by treating 6-methyl-5-[2-(phenoxy)ethyl]-2-thioxo-2,3-dihydro-1H-pyrimidin-4-ones with an excess of aqueous monochloroacetic acid solution. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1213–1217, August, 2005.     

1-{8-甲氧基-2,3-二氢苯并[b][1,4]二噁烷-5-基}乙酮的合成

以邻香兰素为起始原料、经氧化裂解、付克反应及环合反应制得PDE-4抑制剂的中间体1-{8-甲氧基-2,3-二氢苯并[b][1,4]二噁烷-5-基}乙酮,总收率58.9%。     

Proline-Catalyzed Synthesis of 5-Aryl-2-oxazolidinones from Carbon Dioxide and Aziridines Under Solvent-Free Conditions

Natural α-amino acids were proven to be ecofriendly and recyclable catalysts for the carboxylation of aziridines with CO₂ without utilization of any organic solvents or additives. Notably, a series of 5-aryl-2-oxazolidinones were obtained in good yield together with excellent chemo- and regioselectivity under mild conditions using proline as the catalyst. Notably, the catalyst could be recycled more than five times after a simple separation procedure without appreciable loss of catalytic activity. This process represents a promising strategy for homogeneous catalyst recycling.     

Synthesis of N1-Substituted-3-aryl-4-alkyl-4, 5-dihydro-1H-1-pyra-zolethiocarboxamide as Novel Small Molecule Inhibitors of Cysteine Protease of T.cruzi

It has been reported that the pyrazoline scaffold has activity against a broad range of therapeutic targets (e.g antibacterial、antiviral、anti-inflammatary )1,2. In our previous studies of the small molecule inhibitors of cysteine protease of T.cruzi (cruzain), the compounds, 1-(3-bromopropiophenone)-4-subsituted-thiosemicarbazonesVII, have been designed and tested both in vitro as potential antitrypanosomal agents and in the cell culture assay against T. cruzi (the causative agent of Chag…     

5-氨基-1,3-二氢-1,3-二氧-异吲哚-2-丙酸类衍生物的合成及抗血管生成活性研究

根据RGD序列肽的构效关系, 设计并合成了一系列以5-氨基-1,3-二氢-1,3-二氧-异吲哚-2-丙酸为分子骨架的新化合物. 其中间体和目标物的化学结构经¹H NMR, MS和元素分析确证. 体外初步生物活性筛选结果表明, 目标物在10^－5 mol/L浓度下对bFGF诱导的鸡胚绒毛尿囊膜新生血管生成有显著抑制活性.     

3—芳基—5—巯基—1,2,4—均三唑的双—Mannich反应研究

研究了在氯化氢－乙醇溶液中，３－芳基－５－巯基－１，２，４－均三唑与甲醛和伯胺（芳胺或脂肪胺）的双Ｍａｎｎｉｃｈ反应，合成了１３的的稠杂环化合物３，５－二取代０四氢均三唑并「３，４－ｂ」「１，３，５」噻二嗪，经元素分析、Ｉ手ＭＳ确定了结构，初步测定了该类化合物的生物活性。