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1.
Study on the quantitative structure-activity relationship (QSAR) of 26 compounds, N-[5-(2-furanyl)-2-methyl-4-oxo-4H-thieno[2,3-d]pyrimidin-3-yl]-carboxamide and 3-substituted- 5-(2-furanyl)-2-methyl-3H-thieno[2,3-d]pyrimidin-4-ones, with three-dimensional holographic vector of atomic interaction field (3D-HoVAIF) was carried out. SMR-PLS QSAR models have been created and good correlation coefficients and cross-validated correlation coefficients were obtained. The result shows that the models have good prediction capability and favorable stability and the 3D-HoVAIF is applicable to the molecular structural characterization and biological activity prediction. 相似文献
2.
The intramolecular cyclization of 2-(N-acylthioureido)-3-carbethoxy-4,5-R,R'-thiophenes with the formation of potassium salts of 2-thio-4-oxo-5,6-R,R'-3,4-dihydrothieno[2,3-d] pyrimidine was studied, and some of their S-derivatives were obtained. 相似文献
3.
Kut M. M. Onysko M. Yu. Suikov S. Yu. Lendel V. G. 《Russian Journal of Organic Chemistry》2020,56(10):1711-1715
Russian Journal of Organic Chemistry - 3-Phenyl-2-(prop-2-en-1-ylsulfanyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one reacted with 4-methoxyphenyltellurium trichloride in a... 相似文献
4.
Synthesis of 4-amino-6-hetarylthieno[2,3-d]pyrimidines from 5-acetyl-6-aminopyrimidine-4(3H)-thiones
Komkov A. V. Baranin S. V. Dmitrenok A. S. Zavarzin I. V. 《Russian Chemical Bulletin》2022,71(8):1720-1728
Russian Chemical Bulletin - An efficient method for the synthesis of functionalized thieno[2,3-d]pyrimidines and 2-(thieno[2,3-d]pyrimidin-6-yl)pyrido[2,3-d]pyrimidines from... 相似文献
5.
A.-A. S. El-Ahl 《Phosphorus, sulfur, and silicon and the related elements》2013,188(1):189-201
Abstract The synthesis of acetic 2-{[1-methyl-2-(4-oxo-5,6,7,8-tetrahydro-4H-benzo [4,5]-thieno [2,3-d] [1,3-oxazin-2-yl)ethylidene]amino}-4,5,6,7-tetrahydrohenzo[b]thiophene ?3-carboxylic acid anhydride 5 and 2-(oxopropyl)-5,6,7,8-tetrahydro-4H-benzo-[4,5] thieno[2,3-d][1,3]oxazin-4-one 7, has been achieved in three steps from ethyl 2-amino-4,5,6,7-tetrahydrobenzo(b]thiophene-3-carboxlate 1 via the reaction with ethyl acetoacetate followed by hydrolysis and acetic anhydride-induced cyclization. The 2-substituent in compound 5 has two functional groups i.e. active methylene and acid anhydride which are suitably located for intramolecular transformation. Thermal and/or base catalyzed intramolecular cyclization of 5 afforded 2-(4-acetoxy-(hydroxyl)-2-methyl-5,6,7,8-tetrahydrobenzo[4,5] thieno[2,3-b]pyridin-3-yl)-5,6,7,8- tetrahydro-4H-benzo[4,5]thieno[2,3-d] [1,3]oxazin-4-one 10 and 9 respectively. Treatment of 5 with hydrazine hydrate, aromatic and/or heterocyclic amines induced the same intramolecular cyclization with a concomitant oxazine-pyrimidine interconversion to give 3-amino(aryl or heteryl)-2-(4-hydroxy-5,6,7,8-tetrdhydrobenzo-[4,5]thieno[2,3-b]pyridin-3-yl)-3,4,5,6,7,8-hexahydrobenzo[4,5] thieno[2,3-d] pyrimid in-4-one 11–14 respectively. 相似文献
6.
The reaction of 3-(1-hydropolyfluoroalkenyl)-1-oxo-2,4,1-benzoxazines 1 with some dinucleophiles was inves-tigated.7-Fluoroalkyl-2,3-dihydro-1,4-diazepine[1,2-d]quinazolin-11-ones 2,2-fluoroalkylisoxazolo[3,2-b]quin-azolin-9-ones 3 and 2-fluoroalkylbenzoimidazoles 4 were obtained from the reaction of 1 with 1,2-diaminoethane,hydroxylamine hydrochloride and 1,2-diaminobenzene respectively. 相似文献
7.
The synthesis of two new heterocycles is described: pyrido-[2,3-d]-.s-triazolo[ 3,4-f] pyrimidine and pyrido[3,2-d]-.s-triayzolo-[3,4-f] pyrimidine. 4-[I'-Pyrazolyl]pyrido[2,3-d]pyrimidines and 4-[1′-pyrazoly1] pyrido[ 3,2-d] pyrimidine are obtained by the action of 4-hydrazinopyrido[2,3-d]pyrimidine and 4-hydrazinopyrido-[3,2-d]pyrimidine with several β-diketones. 相似文献
8.
Harutyunyan A. A. Israyelyan S. G. Panosyan H. A. Hovsepyan T. R. 《Russian Journal of Organic Chemistry》2020,56(7):1211-1216
Russian Journal of Organic Chemistry - One-pot three-component reactions of 2,6-diaminopyrimidin-4-(3H)-one with aromatic aldehydes and 1- or 2-naphthol afforded benzo[7,8]chromeno[2,3-d]pyrimidine... 相似文献
9.
The bis(carbodiimides) 4, obtained from bis-aza-Wittig reactions of bis(iminophosphorane) 3 with 2 equiv of aromatic isocyanates, were reacted with secondary amine to give symmetrically substituted 2,7-diaminothieno[2,3-d:5,4-d']dipyrimidine-4,5(3H,6H)-dione 6 in the presence of a catalytic amount of EtO(-)Na(+). Reactions of 4 with phenols or ROH in the presence of a catalytic amount of potassium carbonate or RO(-)Na(+) gave symmetrically substituted 2,7-diaryl(alkyl)oxythieno[2,3-d:5,4-d']dipyrimidine-4,5(3H,6H)-diones 6 in satisfactory yields. However, iminophosphoranes 9 were obtained via reaction of bis(iminophosphorane) 3 with 1 equiv of aromatic isocyanate and subsequent reaction with an amine in the presence of a catalytic amount of EtO(-)Na(+). Further reaction of iminophosphoranes 9 with aromatic isocyanates and various nucleophile generated unsymmetrically substituted thieno[2,3-d:5,4-d']dipyrimidine-4,5(3H,6H)-diones 12 in good yields. 相似文献
10.
V. N. Britsun A. N. Esipenko V. V. Piroghenko M. O. Lozinskii 《Chemistry of Heterocyclic Compounds》2008,44(8):979-984
[3+3] Cyclocondensation of 5-benzoyl-3-ethoxycarbonyl-6-methylthio-1-R-1,2-dihydropyrid-2-ones with heterocyclic N,N-and N,C-1,3-dinucleophiles
proceeds regioselectively to give a series of new tri-and tetracyclic heterosystems, viz. derivatives of 5,6-dihydropyrazolo[1,5-a]pyrido[2,3-d]pyrimidin-6-one,
1,2-dihydropyrido[2,3-d]pyrido[2′,3′: 3,4]pyrazolo[1,5-a]pyrimidin-2-one, 8,9-dihydro-5H-pyrido-[2,3-d]thiazolo[3,2-a]pyrimidin-8-one,
1,2-dihydrobenzo[4,5]imidazo[1,2-a]pyrido[2,3-d]pyrimidin-2-one, and 1,2-dihydrobenzo[4,5]imidazo[1,2-g][1,6]naphthyridin-2-one. 相似文献
11.
Max Robba Michel Cugnon de Svricourt Anne-Marie Godard 《Journal of heterocyclic chemistry》1978,15(8):1387-1391
[1] Benzofuro[2,3-d] pyridazone was synthesized by three methods namely8: catalytic dehalogenation of the 4-chlorobenzofuro [2,3-d] pyridazone; removal of the hydrazono group of 4-hydrazinobenzofuro [2,3-d] pyridazine and desulphurization of benzofuro [2,3-d] pyridazine and desulphurization of benzofuro [2,3-d] pyridazine-4(3H) thione. The 4-substituted derivatives were obtained by nucleophilic attack of the 4-chlorobenzofuro[2,3-d] pyridazine. Tetrazolo[1,5-b]- and s-triazolo-[1,2-b] benzofuro [2,3-d] pyridazones. The structural assignment of the benzofuro[2,3-d]pyridazones was made by the Noe effect. 相似文献
12.
S. V. Gorelov S. P. Bondarenko M. S. Frasinyuk 《Chemistry of Heterocyclic Compounds》2012,48(6):955-962
Substituted 4-[(3-cyanopyridin-2-yl)thiomethyl]coumarins have been synthesized by the alkylation of 2-mercapto-4,6-dimethylnicotinonitrile with 4-chloromethylcoumarins. Substituted 4-(3-amino-thieno[2,3-b]pyridin-2-yl)coumarins have been obtained by a subsequent intramolecular condensation of the methylene and cyano groups. 6H-Chromeno[4,3-d]thieno[3,2-b:5,4-b']dipyridin-6-ones were isolated as a result of the interaction of these compounds with aldehydes, and their aminomethyl derivatives were synthesized. 相似文献
13.
El-Sayed H. A. Said S. A. El-Hamid A. Abd Mohamed A. S. A. Amr A. E. Morsy H. A. 《Russian Journal of General Chemistry》2021,91(7):1403-1408
Russian Journal of General Chemistry - Herein, synthesis of a new series of pyrano[2,3-d]pyrimidine scaffolds is presented. Ethyl 6-amino-4-(4-chlorophenyl)-5-cyano-2-methyl-4H-pyran-3-carboxylate... 相似文献
14.
A microscale synthesis (500 mg) of the product 3-[5-anilino-(2,3-d)-dioxole-1,3]-1-oxo-1, 3-dihydro-2-benzofurane (COR.01.126) is described. This method, which requires only four steps, is principally available for the 14C-labeled synthesis with labeled phthalic anhydride as starting material. 相似文献
15.
(2S,3S)-[3-(2)H1]-4-Methyleneglutamic acid 1a and (2S,3R)-[2,3-(2)H2]-4-methyleneglutamic acid 1b have been synthesised for use in biosynthetic and metabolic studies. 相似文献
16.
F. A. Amer M. Hammouda A.-A. S. El-Ahl B. F. Abdel-Wahab 《Chemistry of Heterocyclic Compounds》2007,43(12):1559-1566
New pyrrolo[3,4-c]isoxazole derivatives were synthesized from the key intermediates 4-cyanopyrrolidin-3-ones in two steps.
Pyrrolo[2,3-d][1,2,3]triazoles and triazolo[4,5-c]pyridazine were obtained from 2-arylhydrazono-4-cyano-1-(4′-methoxyphenyl)-3-oxopyrrolidines
by refluxing with phenylhydrazine in either ethanol or glacial acetic acid. Aldol self-condensation of 1-aryl-4-cyanopyrrolidin-3-ones
afforded dipyrrolo-[3,2-b:3′, 4′-d]pyran derivatives.
__________
Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 12, pp. 1841–1848, December, 2007. 相似文献
17.
A novel, efficient, microwave assisted route for the synthesis of 6-substituted-2,3,4-trihydropyrimido[1,2-c]-9,10,11,12-tetrahydrobenzo[b]thieno[3,2-e]pyrimidines in good yields has been developed. The intermediates, 2-substituted-4-[3-hydroxy(propyl-1-amino)]5,6,7,8-tetrahydrobenzo[b]thieno[2,3-d]pyrimidines were obtained by irradiating 2-substituted-4-chloro-5,6,7,8-tetrahydrobenzo[b]thieno[2,3-d]pyrimidines with 1-amino-propanol under basic conditions in a microwave oven. 4-Chlorothieno[2,3-d]pyrimidines were synthesized by microwave irradiation of equimolar mixture of 4-hydroxythieno[2,3-d]pyrimidines and phosphorus oxychloride. The final compounds were screened for antibacterial activity by Kirby Bauer's method using amicacin as the standard against various gram positive and gram negative bacteria. All the compounds showed antibacterial activity comparable with the standard. 相似文献
18.
Refaah A. Alshahrani Adil A. Gobouri Naif A. Alshanbari Saleh A. Ahmed 《Phosphorus, sulfur, and silicon and the related elements》2018,193(6):345-349
The targeted synthesis of 2-(methylsulfanyl)-6-(furan-2-yl)-4(3H)-selenoxo -pyrimidine-5-carbonitrile failed due to the formation 1-methyl-2-methylsulfanyl-6-oxo -4-(furan-2-yl)-1,6-dihydropyrimidine-5-carbonitrile. A new series of 5,6,7,8-tetrahydro-1-benzo thieno[2,3-d]pyrimidine-4-yl substituted selanyl derivatives were prepared by the reaction of sodium diselenide with 4-chloro-5,6,7,8-tetrahydro-1-benzothieno[2,3-d]pyrimidine followed by the reaction with chloroacetic acid derivatives such as ethyl chloroacetate, chloroacetamide or chloroacetonitrile. Hydrazinolysis of ethyl (5,6,7,8-tetrahydro-1-benzothieno[2,3-d]pyrimidine- 4-ylselanyl)acetate with hydrazine hydrate gave the corresponding hydrazino derivative. The latter reacted with ethyl acetoacetate, acetylacetone, diethyl malonate, ethoxymethylenemalononitrile or ethyl 2-cyano-3-ethoxyacetate to afford 5-methyl-2-[2-(5,6,7,8-tetrahydro-1-benzothieno [2,3-d]pyrimidine-4-ylselanyl)acetyl]-2,4-dihydropyrazol-3-one, 1-(3,5-dimethylpyrazol-1-yl)-2- (5,6,7,8-tetrahydro-1-benzothieno[2,3-d]pyrimidin-4-ylselanyl)ethanone, 1-[2-(5,6,7,8-tetrahydro -1-benzothieno[2,3-d]pyrimidine-4-ylselanyl)acetyl]-2,4-dihydropyrazolidine-3,5-dione and 5-Amino-1-[2-(5,6,7,8-tetrahydro-1-benzothieno[2,3-d]pyrimidin-4-ylselanyl)acetyl]-1H-pyrazol -4-yl substituted carbonitrile or ethyl carboxylate, respectively. The structure of the novel compounds was confirmed by spectroscopic tools (IR, 1H NMR 13C NMR and mass spectra) and elemental analysis. 相似文献
19.
XU Jia-xi~** ZUO Gang LIANG Bo Key Laboratory of Bioorganic Chemistry Molecular Engineering of Ministry of Education Department of Chemical Biology College of Chemistry Molecular Engineering Peking University Beijing P. R. China 《高等学校化学研究》2005,21(3)
Introduction Mostimportantantibioticspossessarepresen- tativestructureofaβ-lactamfusedfive-orsix- memberedheterocyclicringcontainingnitrogenand sulfuratoms.Forinstance,theeffectiveantibi- otics,penicillin,penamandpenem,havefusedthi- azolidine-β-lactam,andtheeffectiveantibiotics, cephalosporinandcephem,arefuseddihydroth- iazine-β-lactams[1].Recently,someβ-lactam derivativeshavealsobeenrecognizedasthein- hibitorsofhumanleukocytaseelastase[2]andserine protease[3].Thesynthesisofbicyclicβ-lact… 相似文献
20.
4-Chloro derivatives of thieno[2,3-d]pyrimidine are formed by the action of phosphorus oxychloride on 5-methyl- and 5-methyl-6-carbethoxythieno[2,3-d]pyrimidin-4-ones. Action of nucleophilic reagents (methanol, sodium methylate, primary and secondary amines) on these chloro derivatives gave 4-methoxy-, 4-alkylamino-, and 4-dialkylamino substituted thieno[2,3-d]pyrimidines. It was found that 4-methoxy derivatives of thieno[2,3-d]pyrimidines undergo a thermal rearrangement into 3-methyl-substituted thieno[2,3-d]pyrimid-4-ones. In the bromination of 5-methyl-4-chloro- and 5-methyl-4-methoxy-substituted thieno[2,3-d]pyrimidines by N-bromosuccinimide, 5-bromomethyl derivatives of thieno[2,3-d]pyrimidine are formed, from which, by the action of primary and secondary amines, 5-aminomethyl-substituted thieno[2,3-d]pyrimidines were obtained. A synthesis of 1,2,3,4-tetrahydro-1,3-diazepino[4a,10-d,e] thieno[2,3-d]pyrimidines was also carried out.Deceased.Translated from Khimiya Geterotsilicheskikh Soedinenii, No. 7, pp. 925–928, July, 1985. 相似文献