1,4-氧硫杂萘-4,4-二氧化物含氟衍生物的合成

以含氟的2-(2-氯-4-硝基苯磺酰基)-1-劳基乙酮为原料,在K_OCO_3/TEBA/DMF体系中,与烷基化试剂发生烷基化-环化反应。合成六种未经文献报道的1,4-氧硫杂萘-4,4-二氧化物的含氟衍生物,利用元素分析、IR、~1H NMR、MS对其结构进行了表征。     

The Synthesis and Herbicidal Evaluation of Fluorine-Containing Phenoxyacetoxyalkylphosphonate Derivatives

To investigate the influence of a fluorine moiety on the biological activity of phenoxyacetoxyalkylphosphonates, a series of fluorine-containing phenoxyacetoxyalkylphosphonates were synthesized and screened for herbicidal activity in a greenhouse. The majority of the title compounds showed better preemergence activity than postemergence activity against the test plants, especially on monocotyledon. Compound 5l exhibited notable activity. Results showed that by introducing a fluorine moiety to the parent structure of phenoxyacetoxyalkylphosphonates, a series of new compounds with satisfactory herbicidal activity could be synthesized. A reasonable combination of a fluorine moiety and other substituents on the benzene ring had a great influence on the herbicidal activity.     

Synthesis of 5-Arylisoxazole and 4,5-Dichloroisothiazole Amino-Substituted Derivatives and Their Biological Activity

Russian Journal of General Chemistry - A series of amino derivatives of 5-arylisoxazoles and 4,5-dichloroisothiazole with primary and secondary amino groups was synthesized....     

Synthesis of Novel Imidazole-4,5-Dicarboxamide Derivatives

Imidazolecarboxamide derivatives have been known to exhibit biological activity, especially antiparasitic activity.¹ To date imidazole-4(5)-monocarboxamide derivatives and symmetrical imidazole-4,5-dicarboxamide derivatives have been investigated.¹ However, unsymmetrical imidazole-4,5-dicarboxamide derivatives, having different carboxamide groups, have not been investigated. Therefore, the author was prompted to devise a synthetic method for unsymmetrical diamide derivatives.     

Synthesis and Properties of New Fluorine-Containing Thieno[2,3-b]pyridine Derivatives

Russian Journal of General Chemistry - Cyanothioacetamide reacted with 1,1,5,5-tetrafluoroacetylacetone to give 4,6-bis(difluoromethyl)-2-thioxo-1,2-dihydropyridine-3-carbonitrile, and alkylation...     

无溶剂Ugi四组分反应合成新型含氟Philanthotoxin-12衍生物及杀虫活性

以无溶剂Ugi四组分反应合成关键含氟中间体,然后经三氟乙酸脱除保护基,合成了8个未见文献报道的新型含氟Philanthotoxin-12衍生物。重要的中间体和目标化合物的结构经¹H NMR、¹³C NMR和HRMS或MS的确认。对目标化合物进行了初步的杀虫活性测试,其中含氟的化合物6b在100 mg/L浓度下对棉铃虫和菜青虫的杀死率分别为44%和42%。     

An Efficient Method for the Synthesis of 5-Arylisoxazoles from Benzyl Cobaloximes Using Microwave Irradiation

A new and rapid method is described for the synthesis of 5-arylisoxazoles from benzyl cobaloximes using microwave irradiation.     

1,3-偶极环加成合成新型4,5-二氢-2′,5′-二氧杂吡咯啉并[4,5-c]异噁唑衍生物

N-取代苯基马来酰亚胺与α-氯代-1,2,3-三唑-4-甲醛肟和α-氯代-喹喔啉-2-甲醛肟在三乙胺作用下通过1,3-偶极环加成合成了一系列4,5-二氢-2′,5′-二氧杂吡咯啉并[4,5-c]异(口恶)唑衍生物.化合物结构经元素分析,IR, 1H NMR及MS得到确证.     

Synthesis of 4,5-dihydroisoxazole and isoxazolin-5-ones

The synthesis of 5-hydrazono-4,5-dihydroisoxazoles 3 , from N'-(3-imino-3-aryl-1-methyl-1-alquenyl) hydrazones 1 and hydroxylamine hydrochloride, is described. These 4,5-dihydroisoxazoles can be transformed into oximes 5 and isoxazolones 6 by treatment with reducing agents and ethyl chloroformate, respectively.     

Synthesis and Applications of Selected Fluorine-Containing Fluorophores

The synthesis of fluorine-containing small molecules has had numerous benefits of improving the quality and efficiency of many applications of these compounds. For example, fluorine adds promising functionalities in various areas of imaging (MRI, PET, and NIR); gives cell-targeting properties; and has demonstrated improvements in cell permeability, solubility, and other pharmacologic properties. For these and other numerous reasons, fluorination of molecules has grown in popularity in various fields of chemistry. Many reports show the effects observed from increasing the number of fluorine atoms on a fluorophore scaffold. This report will cover the most significant applications and improvements that fluorine has contributed to in various dye scaffolds such as BODIPY, rhodamine, phthalocyanine, and cyanine in the recent decade.     

Synthesis of New Imidazo[4,5-b]pyridine Derivatives

New imidazo[4,5-b]pyridine derivatives with various substituents in the 2-position (,-unsaturated ketones, imines, ²-pyrazolines, pyrimidines, 1,2,3,4-tetrahydropyrimidines) and derivatives of the new pyrido[3',2':4,5]imidazo[1,2-d][1,2,4]triazine ring system were synthesized. Biological data for selected compounds are presented.     

2-氨基-4,5-二取代烃嘧啶类衍生物的新合成方法

研究了2-氨基-4,5-二烃基取代嘧啶类衍生物的一个新的简易合成方法,该方法以简单且廉价的4个芳香醛和3个脂肪醛为原料,经过四步反应得到12个2-氨基-4,5-二烃基取代嘧啶类化合物,总收率在40%～70%,经氢核磁共振(1H NMR)、碳核磁共振(13C NMR)和高效液质联用(LC-MS)对其目标产物进行表征.     

Synthesis of 2-Cyano-1-(4-nitrophenyl)pyrrole and Its 5-Bromo- and 4,5-Dibromo Derivatives

1-(4-Nitrophenyl)pyrrole-2-carbaldehyde, its 5-bromo-, 4'5-dibromo derivatives react withhydrazoic acid in chloroform in the presence of Mg(ClO₄)₂·2.5H₂O (Schmidt reaction) to form the corre-sponding pyrrole-2-carbonitriles.     

Stereoselective Synthesis of 4,5-Dihydroisoxazole Derivatives from 1,1-Dicyanocyclopropanes and Hydroxylamine Hydrochloride

An efficient approach was developed for the synthesis of 4,5-dihydroisoxazole derivatives from substituted 1,1-dicyano-cyclopropanes and hydroxylamine hydrochloride in ethanol through FeCl₃-catalyzed cascade addition reactions. This procedure gives a useful method to afford stereoselectively poly-substituted 4,5-dihydroisoxazoles in good yields.     

新型含氟1,2,4-三唑[3,4-b]-1,3,4-噻二唑衍生物的合成及其除草活性

以对氟苯甲酰肼为初始原料,经成盐、环化和一锅法反应制得中间体5-对氟苯基-2,4-二氢-1,2,4-三唑-3-硫酮磷亚胺(4);4与芳基异氰酸酯发生氮杂Wittig反应,后经成环反应合成了11个新型的含氟6-芳氨基-1,2,4-三唑[3,4-b]-1,3,4-噻二唑衍生物(6a~6k),其结构经~1H NMR,~(13)C NMR,IR和HR-MS表征。对单、双子叶植物的除草活性测试结果表明:浓度为100 mg·L~(-1)时,6c和6f对稗草和萝卜的茎和根的生长表现出优异的抑制活性,抑制率高达100%。     

5-二茂铁基吡唑啉衍生物的合成及性质

以甲酰基二茂铁和2-乙酰基吡啶为原料, 合成了3个1-芳香酰基-3-(2-吡啶基)-5-二茂铁基-2-吡唑啉衍生物(3~5), 通过红外光谱、质谱、¹H NMR、¹³C NMR和元素分析对其进行了表征, 并对化合物4的单晶结构进行了解析. 研究了该类化合物的电化学性质及紫外、荧光光谱, 并借助密度泛函理论(DFT)计算从理论上加以解释.     

Synthesis of Isatin and 5-Bromoisatin Derivatives

New N-derivatives of isatin were synthesized by treating ethyl chloroacetate, N-(2-chloroethyl)morpholine, and 1,4-di(chloromethyl)benzene with isatin sodium salt. N-Derivatives of isatin and 5-bromoisatin were also prepared by Mannich reaction.     

Synthesis and Photoreaction of 5-Aikenyloxypsoralen Derivatives

Abstract— In order to investigate the intramolecular "quenching" of the photoexcitation of some 5-alkenyloxypsoralen derivatives, we have prepared model compounds in which a psoralen moiety was linked at position 5 to a terminal double bond via a polymethylenic chain of various length (n = 2-9). The isolation and characterization of photocycloadducts obtained for each compound after irradiation at 365 nm in a polar solvent was performed. The results on the photoreactivity of this series of compounds show that the 3,4-pyrone double bond of 5-alkoxypsoralens is the most reactive. Four kinds of intramolecular photocycloadducts between the 3,4-pyrone double bond and the chain unsaturation were obtained according to the length of the linking chain: cis-syn, trans-syn, cis-anti and trans-anti. Their structures were established by a combination of ¹H and ¹³C NMR and fully assigned by ^lH NOE (nuclear Overhauser effect) and ¹H-¹³C HMQC (heteronuclear multiquantum correlation) spectroscopies. No traces of 4',5' adducts were detected.     

Design,Synthesis, and Antifungal Activity of Some New Thiazolo[4,5-d]pyrimidine-5-thione Derivatives

Russian Journal of Organic Chemistry - A new series of thiazolo[4,5-d]pyrimidine-5-thione derivatives having indole and phenyl moieties were synthesized. Their structures were established by...     

Synthesis of Poly-5-vinylindole Derivatives

5-Vinyl-N-benzylindoline and 5-vinyl-N-benzylindole were synthesized starting from the corresponding 5-formyl derivative, by utilizing the Wittig or Wittig-Horner reactions. The monomers were polymerized by free-radical (AIBN) and anionic (BuLi) catalysts. Poly-5-vinyl-N-benzylindole was converted through suitable reactions to the tryptamine and indole acetic acid derivatives. Poly-5-vinyl-N-benzyl-tryptophane was synthesized by malonic ester synthesis by utilizing the condensation of poly-5-vinyl-N-benzylgramine and diethyl formamidomalonate.