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在微波作用、无催化剂的条件下合成3-芳基亚甲基-1,3-二氢-2H-吲哚-2-酮类化合物 总被引:3,自引:1,他引:3
用DMF作溶剂,无催化剂、微波辐射的条件下,使吲哚-2-酮(1)和醛、酮(2)发 生缩合反应,合成了3-芳基亚甲基-1,3-二氢-2H-吲哚-2-酮类化合物,时间短、 收率高。 相似文献
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本文报告了利用磷试剂制备2-氧代-3-甲基-3-异丙基-3H-咪唑并[2,1-a]-1-氧代-异吲哚及其异构体3-氧代-2-甲基-2-异丙基-2H-咪唑并[2,1-a]-1-氧代-异吲哚和2-[4,5-二氢化-4-甲基-4-异丙基-5-氧代-1H-咪唑啉-2-基]-N,N-二烷基-苯甲酰胺的新方法。本文方法具有反应条件温和、反应时间较短和收率较高等特点。 相似文献
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以2-吲哚酮为先导化合物,设计合成一系列2-吗啉基-1-丙基-1H-吲哚-3-取代酰腙类化合物.目标化合物结构经核磁共振波谱(1H NMR和13C NMR)和高分辨质谱仪(HRMS)进行确证.采用浊度法测试了目标化合物的离体抑菌活性,抑菌活性测试结果表明:目标化合物对柑橘溃疡病菌(Xanthomonas axonopodis pv.Citri,X.citri)、烟草青枯病菌(Ralstonia.Solanacearum,R.solanacearum)和水稻白叶枯病菌(Xanthomonas oryzae pv.Oryzae,X.oryzae)均表现出一定的抑制活性.化合物2-氰基-N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)乙酰肼(12a)、4-氯-N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)苯甲酰肼(12c)、4-氟-N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)苯甲酰肼(12f)、N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)-4-硝基苯甲酰肼(12k)和N'-((2-吗啉基-1-丙基-1H-吲哚-3-基)亚甲基)异烟肼(12m)表现出较好的抑制活性;化合物12a、12c、12f、12k和12m对水稻白叶枯病菌的EC50为73.79、61.94、59.70、36.72和82.79μg/m L,抑制活性优于对照药叶枯唑和噻菌铜(EC50分别为92.4、120.22μg/m L). 相似文献
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Pessoa-Mahana H Núñez CU Araya-Maturana R Barría CS Zapata-Torres G Pessoa-Mahana CD Iturriaga-Vasquez P Mella-Raipán J Reyes-Parada M Celis-Barros C 《Chemical & pharmaceutical bulletin》2012,60(5):632-638
A series of 3-[3-(4-aryl-1-piperazinyl)-propyl]-1H-indole derivatives (12a-h) was synthesized and evaluated for binding affinity at the human 5-hydroxytryptamine(1A) receptor (5-HT(1A)R) compounds (12b) and (12h) showed the highest 5-HT(1A) receptor affinity (IC(50)=15 nM). Molecular docking studies with all the compounds in a homology model of 5-HT(1A) showed that the main interaction anchoring the ligand in the receptor was a charge-reinforced bond between the protonated nitrogen atom (N-4) of the piperazine ring and Aspartate(3.32). 相似文献
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Qi CHEN Xing Hai SHEN* Hong Cheng GAO* College of Chemistry Molecular Engineering Peking University Beijing 《中国化学快报》2004,(2)
The hydrophobic cavities of cyclodextrins and the inclusion with various organic molecules in the aqueous solution make them useful in chemical and biological activities1, one of which is the modified cyclodextrins acting as indicators of molecular recognition. Cyclodextrins, which are spectroscopically inert, can be converted into spectroscopically active compounds by modifing one or two of the hydroxy groups with appropriate chromophores, and used as molecular sensor due to the capability of… 相似文献
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Fischer indolisation of 2-aminophenyl ethyl ketone phenylhydrazone using glacial acetic acid saturated with hydrogen chloride as catalyst affords 3-methylindolo(l′:2′-3:4)2-methylquinazoline and 2-(2-aminophenyl)-3-methylindole. The latter compound is autoxidised to 2-(2-amino-phenyl)-3-hydroxy-3-methyl-3H-indole, a reaction which is shown to be dependent upon the presence of the primary amino group at the 2-position of the 2-phenyl substituent and which is much slower than the corresponding autoxidation of 2-(2-hydroxyphenyl)-3-methylindole to 3-hydroxy-2-(2-hydroxyphenyl)-3-methyl-3H-indole previously reported.Nitration of isopropyl phenyl ketone occurs preferentially at the ortho- rather than the meta- positions of the benzene nucleus. 相似文献
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Methyl derivatives of pyrimido[1,2-a]indol-2-one were obtained by the reaction of 2,3,3-trimethyl-3H-indole salts with acrylamide in a proton-containing solvent. The products were condensed with aromatic aldehydes. The interconversion of pyrimido[1,2-a]indol-2-ones and 1-(2-carbamoylethyl)-3H-indolium salts under the influence of acids and bases was studied.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1056–1059, August, 1986. 相似文献
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6-(3-Methyl-but-2-enyl)-1,3-dihydro-indol-2-one, annonidine F [3-[6-(3-methyl-but-2-enyl)-1H-indolyl]-6-(3-methyl-but-2-enyl)-1H-indole], 1H-indole-5-carbaldehyde, 6-(3-methyl-2-butenyl)-1H-indole, 6-(3-methyl-buta-1,3-dienyl)-1H-indole, 6-(4-oxo-but-2-enyl)-1H-indole and 3-geranylindole were isolated from Monodora angolensis (Annonaceae) while 3-(1,1-dimethyl-but-2-enyl)-5-(3-methyl-but-2-enyl)-1H-indole (caulidine A), 4-[3-(1,1-dimethyl-but-2-enyl)-1H-indol-5-yl]-but-3-en-2-one (caulidine B), 5-(3-methyl-2-butenyl)-1H-indole and 5-(3-methylbuta-1,3-dienyl)-1H-indole were obtained from Isolona cauliflora (Annonaceae); structural determination by spectroscopic analysis. Some of the prenylindoles had antifungal and antimalarial activities. 相似文献
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Khaldoun A. Al-Sou’od Mohammad B. Zughul Adnan A. Badwan 《Journal of solution chemistry》2006,35(10):1377-1388
Phase solubility diagrams (PSDs) at 25 ∘C and molecular mechanical (MM) modeling were used to study the aqueous complexation of some 2H- and 3H-indole derivatives with β-cyclodextrin (β-CD). Among the 3H-indole derivatives investigated in this work, indole-3H-butyric acid forms the most stable 1:1 complex of the B
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-type PSD, whereas shorter chain derivatives form soluble 1:1 complexes (A
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-type PSDs) with their stability increasing as the chain length increases. Indole-2 carboxylic acid forms highly stable 1:1 and 1:2 complexes, with the lower-order complex reaching saturation first (B
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-type PSD). MM modeling indicates that the stability of the complex is highly correlated with the flexibility of the 3H-indole hydrocarbon chain, which yields a better geometrical fit within the β-CD cavity resulting from different hydrophilic interactions. These interactions are represented in the H-bonding of the carboxyl group with the primary hydroxyl group network that is situated at the narrow rim of the cavity, and also by a favorable interaction of the aromatic ring with the hydroxyl group network at the other rim. 相似文献
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An effective synthesis of 1-(6-hydroxyindol-1-yl)-2,2-dimethylpropan-1-one (4) was developed starting from 1H-indole (2). The key step involved suitable utilization of 4-(1-pyrrolidino)pyridine for the removal of the chloroacetyl moiety from chloroacetic acid 1-(2,2-dimethylpropionyl)-1H-indol-6-yl ester (3); a possible mechanism is, also, presented. Compound 4 might lead to selectively substituted derivatives, either on the phenolic-OH or the indolyl-NH, with putative biological interest. In this respect, we found that the core structure of 1H-indol-6-ol (1) possesses a degree of aldose reductase inhibitory potential, at a concentration of 100 microM. 相似文献
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A variety of nucleophiles provided by activated methylenes have been added on 3-(2-nitrovinyl)-1H-indole in very good to excellent yields, under sonication and solvent-free conditions, using solid potassium carbonate or sodium acetate as a base. Direct synthesis avoiding preliminary NH protection is reported and exemplified to 15 molecules. 相似文献
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Tandem reaction of 2-(2-(alkynyl)benzylidene)malonate with indole was investigated. (Z)-1-Benzylidene-3-(1 H-indol-1-yl)-1 H-indene-2,2(3 H)-dicarboxylate was generated in the presence of t-BuOK at room temperature; whereas 3-((1 H-indol-3-yl)(2-(alkynyl)aryl)methyl)-1 H-indole was obtained when Sc(OTf)3 was utilized as catalyst at 50 degrees C. 相似文献
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Kitano M Kojima A Nakano K Miyagishi A Noguchi T Ohashi N 《Chemical & pharmaceutical bulletin》1999,47(11):1538-1548
A series of N-(aminoiminomethyl)-1H-indole carboxamide derivatives were synthesized and their inhibitory potencies against the Na+/H+ exchanger were measured. Variation of the carbonylguanidine group at the 2- to 7-position of the indole ring system showed that a substitution at the 2-position improved the Na+/H+ exchanger inhibitory activity the most in vitro. This led to the synthesis and evaluation of an extensive series of N-(aminoiminomethyl)-1H-indole-2-carboxamide derivatives. Derivatives having an alkyl or substituted alkyl group at the 1-position of the indole ring system showed higher levels of in vitro activities. N-(aminoiminomethyl)- 1-(2-phenylethyl)-1H-indole-2-carboxamide (49) had the strongest activity. 相似文献