共查询到20条相似文献,搜索用时 15 毫秒
1.
Francesco Savelli Alessandro Boido Iana Vazzana Fabio Sparatore 《Journal of heterocyclic chemistry》1987,24(6):1709-1716
In pursuing the study on compounds obtained by condensation of N-monoalkylated aromatic and hetero-aromatic diamines with α- and β-ketoesters, 7,8,9,10-tetrahydrocyclopenta[e]pyrido[3,2-b][1,4]diazepin-6(5H)-ones 4a, 4b and 5,7,8,10-tetrahydrocyclopenta[e]pyrido[2,3,-b][l,4]diazepin-9H)-ones 5a, 5b were prepared starting from 2,3-diaminopyridine or 2,3-diamino-5-chloropyridine and ethyl 2-oxo-cyclopentanecarboxylate. Compounds 4a,b and 5a,b suffer thermally induced ring contraction to the imidazolone derivatives 8a,b and 7a,b respectively and are unsuitable for preparing diazepinone derivatives. Thus the methylated diazepinones 15, 17 and 18 , stable on heating, were prepared. Compound 17 was transformed into the clozapine analogue 22 , through the diazepinthione 20 and its S-methyl derivative 21 . 相似文献
2.
3.
Pyrido‐anellated compounds analogous to tricyclic 1,4‐benzothiazine derivatives were synthesized. Thus, under mild reaction conditiones substitution of thiolactim 3 with different N‐nucleophiles yielded the precursors for compounds, which were cyclized in a further step to the corresponding tricyclic derivatives. 相似文献
4.
Sergey V. Popil'nichenko Vladimir S. Brovarets Alexander N. Chernega Denis V. Poltorak Boris S. Drach 《Heteroatom Chemistry》2006,17(5):411-415
Readily available 2‐acylamino‐3,3‐dichloroacrylonitriles are sequentially treated with methyl mercaptoacetate in the presence of sodium methylate and with sulfuric acid to furnish the methyl ester of 7‐amino‐2‐oxo‐3H‐thieno[2,3‐b][1,4]thiazine‐6‐carboxylic acid. Treating it first with triethyl orthoformate and then with ammonia or primary amines, the pyrimidine‐4‐one nucleus is annelated to the thienothiazine system, which is corroborated by spectroscopic methods and X‐ray diffraction analysis. © 2006 Wiley Periodicals, Inc. Heteroatom Chem 17:411–415, 2006; Published online in Wiley InterScience ( www.interscience.wiley.com ). DOI 10.1002/hc.20232 相似文献
5.
6.
Moustafa A. Gouda 《Journal of heterocyclic chemistry》2011,48(1):1-10
This review describe the synthesis and reactions of 3‐amino‐4,6‐dimethyl‐1H‐pyrazolo[3,4‐b]pyridine as building block for the synthesis of polyfunctionalized heterocyclic compounds with pharmacological interest. J. Heterocyclic Chem., 2011. 相似文献
7.
Francesco Savelli Alessandro Boido Sonia Piacente 《Journal of heterocyclic chemistry》2001,38(3):659-662
With a continuing interest in heteropolycyclic systems which may show biological activities, we studied the reaction of 3‐amino‐2‐(methylamino)pyridine with diethyl 1,3‐acetonedicarboxylate in order to develop pyridodiazepinone derivatives. From the reaction mixture, we separated dipyrido[1,2‐a:2′,3′‐d]imidazole derivatives ( 3 and 4 ) besides two isomeric pyrido[2,3‐b][1,4]diazepine derivatives ( 5 and 6 ) in which the complex structural differentiation was achieved through nmr experiments and chemical evidence. Several attempts to elaborate isomers 5 and 6 have not yet given significant results. 相似文献
8.
Toshiyuki Kohara Hiroshi Tanaka Koreichi Kimura Hideki Horiuchi Kohji Seio Masafumi Arita Tetsuya Fujimoto Iwao Yamamoto 《Journal of heterocyclic chemistry》2002,39(1):163-171
A new series of 4‐(4‐methylpiperazin‐1‐yl)thieno[2,3‐b][1,5]benzoxazepines 1a‐k has been synthesized from 4‐bromo‐2‐methylthiophene 6 or ethyl 2‐amino‐4,5‐dimethyl‐3‐thiophencarboxylate 10 . Preparation of the key intermediate thieno[2,3‐b][1,5]benzoxazepine‐4(5H)‐ones 4a‐i, 4k were carried out by treatment of 2‐bromo‐N‐(2‐hydroxyphenyl)‐3‐thiophencarboxamides 5a‐i, 5k with potassium carbonate in DMSO. Compounds 1 are thienoanalogues of loxapine, a potent antipsychotic drug. Of these compounds, the neu‐roleptic activity of 2‐methyl‐4‐(4‐methylpiperazin‐l‐yl)thieno[2,3‐b][1,5]benzoxazepine 1a (R1, R3=H, R2=CH3) demonstrated potent antipsychotic activity. 相似文献
9.
Cho SD Park YD Kim JJ Lee SG Ma C Song SY Joo WH Falck JR Shiro M Shin DS Yoon YJ 《The Journal of organic chemistry》2003,68(20):7918-7920
Pyrido[2,3-b][1,4]oxazin-2-ones are conveniently prepared in excellent yields by a one-pot annulation of N-substituted-2-chloroacetamides with 2-halo-3-hydroxypyridines with use of cesium carbonate in refluxing acetonitrile. The key transformation features a Smiles rearrangement of the initial O-alkylation product and subsequent cyclization. 相似文献
10.
Abderrahman El Bouakher Hélène LaborieMina Aadil Ahmed El HakmaouiSaid Lazar Mohamed Akssira Marie-Claude Viaud-Massuard 《Tetrahedron letters》2011,52(39):5077-5080
A convenient synthesis of a series of pyrido[3,2-e][1,4]-diazepine-2,5-diones 8 and pyrido[2,3-e][1,4]diazepine-2,5-diones 9, is reported using the condensation of α-amino acid methyl ester derivatives with 1H-pyrido[3,2-d][1,3]oxazine-2,4-dione and 1H-pyrido[2,3-d][1,3]oxazine-2,4-dione. Compounds 8 and 9 were also synthesized by peptide coupling of α-amino acid methyl ester derivatives with β-amino acids (2 or 3) followed by the cyclisation in tetrahydrofuran with sodium hydride (NaH). 相似文献
11.
Derivatives of thiophene, thieno[2,3‐b]pyridine, thieno[5′,4′:4,5]pyrimido[3,2‐a]pyridine and thiepine fused with octyl ring have been synthesized and tested for antimicrobial and antifungal activities. The structure of the newly synthesized compounds have been established on the basis of their analytical and spectral data. 相似文献
12.
Miguel F. Braa 《Journal of heterocyclic chemistry》2003,40(5):917-923
The synthesis of new ligands for the H3 histamine receptor is described. These new compounds are spinacine derivatives obtained by alkylation or Michael reaction at C6 position. 相似文献
13.
N. A. Hassan M. I. Hegab F. M. Abdel‐Motti S. H. A. Hebah F. M. E. Abdel‐Megeid A. I. Hashem 《Journal of heterocyclic chemistry》2007,44(4):775-782
Reaction of 6‐amino‐2‐methylthiouracil and 6‐amino‐1,3‐dimethyluracil with equimoler amounts of cyclic ketones or cyclic 1,3‐diketones and the appropriate aromatic aldehydes yielded regioselectivity a series of polycyclic pyrimido[4,5‐b]quinoline and pyrido[2,3‐d]pyrimidine derivatives in good yields. 相似文献
14.
Marina Kopp Jean‐Charles Lancelot Saïd Dagdag Hugues Miel Sylvain Rault 《Journal of heterocyclic chemistry》2002,39(5):1061-1064
The quasi‐one pot synthesis of new 2‐aminopyrido[1,2‐a][1,3,5]triazin‐4‐ones starting from 2‐amino‐pyridine and 2‐aminopicolines is herein described in order to obtain a library of cyclic guanidines. 相似文献
15.
Derivatives of thieno[2,3‐b]pyridine, 2‐thienylthiourea, 2‐thienylurea, 2‐thienylacetamide incorporating the 2‐phthalimidomethyl moiety have been synthesized. The synthesized compounds were then investigated for antibacterial activity against Escherichia coli, Bacillus subtilis and Staphylococcus aureus. The compounds were also investigated for antifungal activity against Aspergillus niger and Fusarium oxysporium. The structures of the newly synthesized compounds have been established on the basis of their analytical and spectral data. 相似文献
16.
Kurissery A. Tony Santhosh Kumar Chittimalla G. Abraham Rajkumar Anjan Chakrabarti 《Tetrahedron letters》2010,51(33):4350-4353
2-Chloropyridines and an aryl bromide underwent palladium-catalyzed intramolecular C-O bond forming reactions to provide 2,3-dihydrospiro[1,4]dioxino[2,3-b]pyridine derivatives and a benzodioxin, regioselectively. 相似文献
17.
Stephen P. Stanforth 《Journal of heterocyclic chemistry》2005,42(4):723-725
The 2,3‐dihydro‐7‐methyl‐1H,5H‐pyrido[3,2,1‐ij]quinoline‐1,5‐dione derivatives 9 and 10 were prepared from 3‐(5,7‐dimethoxy‐4‐methyl‐2‐oxo‐2H‐quinolin‐1‐yl)propionitrile ( 6 ). Cyclodehydration of the amide 8 gave 1,2‐dihydro‐7,9‐dimethoxy‐6‐methylpyimido[1,2‐a]quinolin‐3‐one ( 11 ). 相似文献
18.
Short Synthesis of Enantiopure Thieno[2,3‐f]triazolo[1,5‐a][1,4]diazepines and Thieno[2,3‐f][1,4]diazepin‐5‐ones 下载免费PDF全文
Giorgio Molteni 《Journal of heterocyclic chemistry》2014,51(Z1):E329-E331
Starting from 2‐carboxy‐3‐thenylazide 1 and enantiopure amines 2 as the chiral building blocks, we developed a two‐step synthesis of the title compounds involving an intramolecular azide cycloaddition as the key step. 相似文献
19.
Synthesis of Imidazo[2,1‐b][2H‐1,3,4]thiadiazines and 1,2,4‐Triazolo[3,4‐b][2H‐1,3,4]thiadiazines 下载免费PDF全文
Stefanie Knak Wolf‐Diethard Pfeiffer Horst Dollinger Ashot S. Saghyan Peter Langer 《Journal of heterocyclic chemistry》2015,52(2):463-467
Imidazo[2,1‐b][2H‐1,3,4]thiadiazines were prepared by cyclization of 2‐amino‐5‐(4‐chlorophenyl)‐6H‐1,3,4‐thiadiazine with α‐haloketones. 1,2,4‐Triazolo[3,4‐b][2H‐1,3,4]thiadiazines were prepared by cyclization of 4‐amino‐5‐sulfanyl‐l,2,4‐triazoles with phenacyl bromides. 相似文献
20.
A new synthesis of 6‐carbomethoxy‐1,2,3,5‐tetrahydroirnidazo[2,3‐b][1,3]benzodiazocines 13 by the intramolecular cycloaddition reaction of methyl 2‐(1‐aziridinylmethyl)‐3‐(2‐ureidophenyl)propenoates 10 under Appel's dehydration conditions is described. The latter were readily obtained from 2‐nitrobenzalde‐hyde with methyl acrylate through the Baylis‐Hillman reaction. 相似文献