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为了寻找新的含苯并噻唑稠杂环农药先导化合物,利用取代2-肼基苯并噻唑与取代苯甲酸在三氯氧磷中回流反应,合成了18个新型取代3-芳基-1,2,4-三唑并[3,4-b]苯并噻唑化合物,并利用1H NMR,EI-MS及元素分析对其结构进行了表征.初步生物活性试验结果表明,在50 mg/L浓度下,部分目标化合物对立枯丝核菌(Rhizoctonia solani)、西瓜壳二孢菌(Ascochyta citrullina)、香蕉枯萎病菌(Fusarium oxysporum f.sp.cubense)、烟草炭疽病菌(Colletotrichum nicotianae)具有中等杀菌活性.然而,部分化合物对灰葡萄孢菌(Botrytis cinerea)反而起到一定促进生长作用. 相似文献
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利用L-脯氨酸催化的5-氯水杨醛(1)与6-甲基-4-羟基吡喃酮(2)的缩合反应及硫酸铜催化下与1,3-二甲基-5-氨基吡唑(3)的串联反应,合成得到了10-氯-1,3-二甲基-5-(2-氧代丙基)色烯并[4,3-d]吡唑并[3,4-b]吡啶-6(3H)-酮(4)和10-氯-5-二乙氧基甲基-1,3-二甲基色烯并[4,3-d]吡唑并[3,4-b]吡啶-6(3H)-酮(5).化合物5的结构通过单晶X射线衍射法确定:晶体属于三斜晶系,空间群P-1;相对分子质量Mr=803.68;晶胞参数a=1.03160(10)nm,b=1.42900(13)nm,c=1.44268(15)nm;V=1.9448(3)nm~3;Z=2;晶胞密度Dc=1.372g/cm~3;吸收系数μ=0.228mm-1;单胞中电子的数目F(000)=840.晶体结构用直接法解出,经全矩阵最小二乘法对原子参数进行修正,最终的偏离因子为R=0.0681,w R=0.2051.在晶体结构中色烯环与吡啶环及吡唑环近似于共平面. 相似文献
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利用3-芳基-4-氨基-5-巯基-1,2,4-均三唑和对氯苯甲酰异硫氰酸酯在乙腈中反应, 得到一系列3-芳基-6-对氯苯甲酰氨基均三唑并[3,4-b]-1,3,4-噻二唑, 用1H NMR, IR, MS和元素分析确定了其结构, 并对其进行了抑菌活性测试. 相似文献
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建立了一种构建八氢吡咯并[3,4-c]吡咯烷类化合物母体双环结构的快速有效方法。以苄胺为原料,与氯甲基三甲基硅烷反应制得仲胺化合物(2);2与甲醇和甲醛反应得亚甲胺叶立德前体化合物(3);在三氟乙酸的诱导作用下,3与马来酰亚胺经1,3-偶极环加成反应得顺式加成产物(4);4经氢化铝锂还原得5-苄基八氢吡咯并[3,4-c]吡咯(5);5经Boc保护氨基后用氢氧化钯碳催化加氢脱苄合成了八氢吡咯并[3,4-c]吡咯-2-碳酸叔丁酯,总收率35%,其结构经1H NMR,IR和MS确证。 相似文献
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在超声波辐射下, 芳香醛、1,3-环己二酮和2-氨基苯并咪唑3组分在离子液体([bmim]Br)介质中经Biginelli反应“一锅煮”合成了一系列新型苯并咪唑并[2,1-b]喹啉-6-酮衍生物. 2-氨基苯并咪唑的使用是对经典的Biginelli反应的发展, 并且该方法具有反应条件温和、产率较高(65%~86%)及环境友好等优点. 产物经IR, 1H NMR和元素分析确证了结构. 相似文献
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M. Anzini A. Cappelli S. Vomero A. Cagnotto M. Skorupska 《Journal of heterocyclic chemistry》1992,29(5):1111-1115
The reaction of 2-chloromethyl-3-ethoxycarbonyl-4-phenylquinoline with phenylhydrazine, afforded 2,3-dihydro-9-phenyl-2-phenylamino-1H-pyrrolo[3,4-b]quinolin-1-one derivatives 2 along with a major amount of 3-ethoxycarbonyl-4-phenylquinoline-2-carboxaldehyde phenylhydrazone 4a . The geometric isomers of phenylhydrazone 4a , displaying solvent-dependent E-Z isomerism, were isolated, characterized by 1H-nmr and mass spectra, and the Z-form easily cyclized to pyridazino[4,5-b]quinoline derivative 5a . Analogously, compounds 2b, 2c, 4b , 4c, 5b and 5c were obtained. The title compounds were tested as potential ligands for central and peripheral-type of benzodiazepine receptors, and the results are reported. 相似文献
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The reaction of N-acetylindoxyl hydrazone with ketones in alcohol gave N-acetylindoxyl alkylindenehydrazones, which were converted to pyrrolo[3,2-b]indole derivatives by treatment with glacial acetic acid. Pyrrolo[3,2-b]indole derivatives were also obtained in the reaction of N-acetylindoxyl hydrazone with ketones in glacial acetic acid. The structures of the synthesized products were confirmed by data from the IR, UV, PMR, and mass spectra.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 201–205, February, 1982. 相似文献
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A. Shafiee M. A. Ebrahimzadeh J. Shahbazi S. Hamedpanah 《Journal of heterocyclic chemistry》1998,35(1):71-75
Starting from the readily available aryl 2-methyl-5-phenyl-3-furyl ketones, 5-methyl-1H-1-phenylpyrazole-4-yl ketones and 4-methyl-2-phenyl-5-thiazolylcarboxaldehyde, a series of 2-phenyl-4-arylthieno[3,4-b]-furan, 2-phenyl-4-(p-methoxyphenyl)selenolo[3,4-b]furan, 4-aryl-1H-1-phenylthieno[3,4-c]pyrazole and 5-benzyl-2-phenylpyrrolo[3,4-d]thiazole were prepared in high yield. 相似文献
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This paper describes the synthesis of a new series of 4-amino-1-(unsubstituted and chloro or fluoro substituted benzyl)-7,8-dihydro-6H-pyrazolo[3,4-b]quinolin-5-ones 8 and the corresponding 7,8-dihydro-6H,9H-pyrazolo[3,4-b]quinoline-4,5-diones 13 . The derivatives obtained by reaction of these compounds with sodium azide in concentrated sulfuric acid are also reported. 相似文献
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A novel multicomponent synthesis of 5-aminooxazole starting from simple and readily available inputs is described. Thus, simply heating a methanol solution of an aldehyde 3, an amine 4, and an alpha-isocyanoacetamide 5 provided the 5-aminooxazole (1) in good to excellent yield. The reaction of 1 with alpha,beta-unsaturated acyl chloride 13 lead to the formation of pyrrolo[3,4-b]pyridin-5-one (2) in a single operation. A triple domino sequence, acylation/IMDA/retro-Michael cycloreversion, is involved in this new scaffold-generating reaction. After the observation that ammonium chloride can significantly accelerate the oxazole formation in toluene, a one-pot four-component synthesis of 2 is developed. 相似文献
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R. G. Glushkov I. M. Zasosova I. M. Ovcharova 《Chemistry of Heterocyclic Compounds》1977,13(10):1122-1126
The reaction of enamines of some -oxo lactams with 1,3-dimethyl- and 1,3-dibenzyl-4-hydrazinouracils gave the uracilyl-4-hydrazones of these lactams, the catalytic and thermal indolization of which yielded derivatives of pyrido[3,4-b]- and azepino[3,4-b]pyrrolo[2,3-d]pyrimidines. Some reactions of the latter were studied.Communication XXVIII from the series Investigation of Lactams. See [1] for communication XXVII.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1398–1403, October, 1977. 相似文献
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3-Aminocoumarin undergoes the Skraup reaction to give a new ring system, 5H[l]benzo-pyrano[3,4-b]pyridin-5-one (IVa). When 3-aminocoumarin was condensed with the ethoxy methylene derivatives of active methylene compounds, ethyl acetoacetate, and dimethyl acetylenedicarboxylate, the intermediates Vla-VIf were formed which on thermal cyclizations afforded other derivatives of 5H[l ]benzopyrano[3,4-b]pyridin-5-one (IVb-IVf). The nitration of IVa gave IVg. 相似文献
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Dario Giardina Roberto Ballini Marcello Ferappi Giovanni Casini 《Journal of heterocyclic chemistry》1978,15(6):993-995
The: title compounds were prepared from Michael adducts, obtained from acetoacetic esters and trans-3-hexene-2,5-dione, and from the corresponding dehydration products, by direct cyclization to oxygen rings or by reaction with ammonia (or methylamine) to give nitrogen rings. 相似文献
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A. V. Eremeev V. G. Andrianov I. P. Piskunova 《Chemistry of Heterocyclic Compounds》1978,14(5):500-502
Various furazano [3, 4-b] pyrazine derivatives were synthesized by condensation of 3, 4-diaminofurazan with substituted phenylglyoxals, cyclic di- and triketones, and diethyl acetylenedicarboxylate.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 5, pp. 613–615, May, 1978. 相似文献