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1.
Yu Xin LIU Xiao Tian LIANG* Institute of Materia Medica Chinese Academy of Medical Sciences &Peking Union Medical College Xian NongTan Street Beijing 《中国化学快报》2001,(1)
In our research on the ring enlargement of certain N-heterocycles, a general procedure for the ring enlargement with the insertion of an extra -CH2- was improved and shown in Scheme I1.Scheme IThe procedure had been carried out with such N-heterocycles as 2-methyl-1,2,3,4-tetrahydroisoquinoline2, tetrahydroberberine and strychnine3 with expected results. Thus, the procedure shown in Scheme I provides a new approach to the synthesis of larger N-heterocycles.Isoindolo[1,2-b][3]benzazepines a… 相似文献
2.
<正>Reactions of the 6-hydroxy-thiopyrano[3,4-c]pyridine-5-carbonitrile derivative 1 withα-halo-carbonyl compounds gave the ortho-substituted intermediates 2a-c which were converted into furo[2,3-b]thiopyrano[4,3-d]pyridines 3a-c by fusion of a furan moiety under basic conditions.Further cyclization of 3a-c led to a fusion of a pyrimidine ring,yielding the tetracyclic products 6,7 and 8.In addition,condensation of 6 with various aromatic aldehydes afforded the corresponding imines 9a,b.Mannich reaction of 7 gave products 10a,b. 相似文献
3.
1INTR0DUCTI0NBenzoheteroazepinecompoundsareimportantpharmaceuticalagents"-".Inre-centyears,ithasbeenfoundthatbenzoheter0azepinetricyclicderivatives,especiallythosefusedwithotherfiveorsix-memberedheterocycle,area1soofpotentialphar-maceuticalinterestst4-6j.Hence,muchattentionhasbeenpaidtothesynthesesofthem,suchasl,3-oxazino[3,2-djt1,5jbenzothia/diazepin-l-onet"'J,1,2,4-tria-zolo[4,3-dj[1,5jbenzothia/diazepine"',1,2,4-oxadiazolo[4,5-dj[l,5jbenzothia/diazepine',',andsoon.Meanwhiletheirstructur… 相似文献
4.
Xu-Sheng Du Dr. Ying Han Prof. Dr. Chuan-Feng Chen 《Chemistry (Weinheim an der Bergstrasse, Germany)》2022,28(3):e202104024
Chiral pseudo[1]rotaxanes and [1]rotaxanes constructed from macrocyclic arenes still remain a big challenge mainly owing to the lack of such chiral macrocycles. In this work, a new system of chiral pseudo[1]rotaxanes formed by self-inclusion of helic[6]arene containing amide linked with the terminal tertiary amines was first discovered. Based on an atom-economic stopping strategy, a pair of chiral [1]rotaxanes were conveniently obtained in almost quantitative yields by blocking the pseudo[1]rotaxanes with monobenzyl bromide of tetraphenylethene. The structures of pseudo[1]rotaxanes and [1]rotaxanes were characterized by 2D NMR spectra in solution, combined with DFT calculations. The photophysical properties further revealed the efficient chirality transfer of helic[6]arene to the tetraphenylethene moiety, compared to their unthreaded chiral isomers. The discovery of the chiral pseudo[1]rotaxanes allows for a wide and available synthesis of chiral [1]rotaxanes, and also opening a new avenue to the design of chiral supramolecular materials. 相似文献
5.
L. Bukowski Zofia Zwolska Ewa Augustynowicz-Kopeć 《Phosphorus, sulfur, and silicon and the related elements》2013,188(7):879-887
Abstract The reactions of 2-cyanomethyl-1-methyl-1H-imidazo[4,5-b]pyridine with isothiocyanates, nitroso compounds, acid chlorides, and thioglycolic acid were investigated. New imidazo[4,5-b]pyridine derivatives with various substituents in 2-position and derivatives of the new pyrrolo[2′,1′:2,3]imidazo[4,5-b]pyridine ring system were synthesized. The compounds obtained were tested in vitro for their tuberculostatic activity. 相似文献
6.
E. Yu. Kambulov V. K. Vasilin E. A. Kaigorodova L. D. Konyushkin G. D. Krapivin 《Chemistry of Heterocyclic Compounds》2003,39(2):255-266
Derivatives of a new heterocyclic system - benz[4,5]imidazo[1,2-c]pyrido[3',2';4,5]thieno[2,3-e]pyrimidine have been obtained by successive reactions in three stages - alkylation of 3-cyanopyridine-2(1H)-thiones with 2-chloromethylbenzylimidazole to give 2-benzimidazolylmethylthio-3-cyanopyridines, closing the thiophene ring in the latter to form 3-amino-2-(benzimidazolyl-2)thieno[2,3-b]pyridines, and cyclization of the pyrimidine ring by acylation with carboxylic acid anhydrides or chlorides. 相似文献
7.
SONGHong-rui WANGFei LIJian ZHANGShou-fang 《高等学校化学研究》2005,21(4):460-462
The three title compounds were prepared from 2-phenylaminomethyl-3H-1,2-dihydro-l-pyrrolizinols via an intramolecular Friedel-Crafts reaction. 2-Phenylaminomethyl-3H-1,2-dihydro-1-pyrrolizinols were prepared from 2-phenyl-aminomethyl-3H-1,2-dihydro-1-pyrrolizinones via reduction. The heterocyclic ring system of pyrrolizino[2,1-c] quinoline has not been found in literature. 相似文献
8.
Afshin Yazdani-Elah-Abadi Malek-Taher Maghsoodlou Razieh Mohebat Reza Heydari 《中国化学快报》2017,28(2):446-452
A green, convenient, high yielding and one-pot procedure for the synthesis of novel spiro[benzo[a]pyrano[2,3-c]phenazine] derivatives by domino multi-component condensation reaction between 2-hydroxynaphthalene-1,4-dione, benzene-1,2-diamines, ninhydrine, and malononitrile in the presence of a catalytic amount of 1,3-dimethyl-7H-purine-2,6-dione (theophylline) as an expedient, eco-friendly and reusable solid base catalyst under thermal, microwave irradiation and solvent-free conditions. This procedure has also been applied successfully for the synthesis of benzo[a]pyrano[2,3-c]phenazines. 相似文献
9.
通过三组份串联反应合成一系列咪唑[1,5-a]吡啶鎓盐,利用1H NMR、13C NMR、MS以及X射线单晶衍射确定其结构,其中以二乙烯三胺与三乙烯四胺为原料获得预期外的结构。以青霉素作为对照,研究了化合物的抗菌性。结果表明,所合成的化合物对溶壁微球菌和乙型链球菌均有抗菌效果,化合物2的抗菌效果最好;含有杂原子O的化合物3对嗜麦芽单胞菌和肺炎克雷伯氏菌的抗菌能力优于青霉素;联苯桥联的刚性双齿咪唑[1,5-a]吡啶鎓(5)比乙基桥联的柔性双齿咪唑[1,5-a]吡啶鎓(4)的抗菌性更强;化合物6为单齿大π体系芳香环,其抗菌效果较好,而化合物7和8为双齿的大π体系芳香环,其抗菌效果较弱。 相似文献
10.
Claudia Tauber Manfred Klade Heinz Sterk Hans Junek 《Monatshefte für Chemie / Chemical Monthly》1990,121(4):299-309
Summary 2,3-Dihydro-3-oxo-benzo[b]thiophen-1,1-dioxide (1) reacts as CH-acidic component with amidines of orthoesters and anilines resp. to give the anilinomethylene derivates3, 4, and5. With triethyl orthoformiate the hydroxymethylene-compound7 is obtained. Anilino- and phenylhydrazino derivates8 and9 prove the carbonyl activity of1, azo-coupling leads to10, whereas treatment of1 with sulfur and malononitrile yields the benzo[b]thieno[2,3-d]thiophenes11. Introduction of substituents with active NH-functions in position 2 of the dicyanomethylene-product2, such as azocoupling, reaction with phenyl isocyanate and formation of enamines, leads to ring closure reactions between a nitrile and the NH-group. Thereby the phenyl-benzo[4,5]thieno[2,3-c]pyridazines12, the phenyl-1H-benzo[4,5]thieno[2,3-c]pyridines13 and the phenylamino-benzo[4,5]thieno[2,3-c]pyridines14 are obtained.13C and15N-NMR spectroscopy was used as proof of the ring closure reactions. 相似文献
11.
Katherine Buggle Úna Ní Ghógáin Patrick MacManus 《Monatshefte für Chemie / Chemical Monthly》1988,119(8-9):945-951
The conversion of 2H-[1]benzothieno[3,2-b]pyran-2-ones into mono- and dithio-derivatives and the preparation of some dibenzothiophenes, sulphines and pyridones are described.
Einige Reaktionen von 2H-[1]Benzothieno[3,2-b]pyran-2-onen und verwandten Verbindungen
Zusammenfassung Es wird die Umsetzung von 2H-[1]benzothieno[3,2-b]pyran-2-onen zu Monound Dithio-Derivaten und die Darstellung einiger Dibenzothiophene, Sulfine, und Pyridone beschrieben.相似文献
12.
Intramolecular cyclization of 1-amino-3-phenacyl-4-carbohydrazido-1,2,3-triazolium-5-olates has been shown to take place via selective interaction of the carbonyl group with the terminal amino function of the hydrazido group to form a 1,2,5-triazepine ring. Minor products, resulting from the interaction of the α-nitrogen atom of the hydrazido group with the carbonyl function, having a N-amino-pyridazine structure were also detected and isolated. A general method for the synthesis of novel mesoionic 2-amino-7-aryl-4-oxo-2,4,5,8-tetrahydro[1,2,3]triazolo[5,1-d][1,2,5]triazepin-9-ium-3-olates was developed. 相似文献
13.
Intermolecular couplings versus intramolecular ring closures were observed in the reaction of p-tert-butylthiacalix[4]arene and diethylene glycols affording dimers 2 and/or the inherently chiral 1,2-thiacalix[4]crown-3 derivatives 5 under the Mitsunobu protocol. The enantiomeric separation of 5a was achieved by chiral HPLC. The reaction of thiacalix[4]monocrowns 1 with diethylene glycols failed to give crowned thiacalix-tubes 7, instead biscrowns 8 were formed. Partially alkylated double thiacalix[4]arenes 10, 11 were obtained via the base promoted alkylations of a thiacalixarene dimer 2a containing diethyleneoxy linkers. 相似文献
14.
Andrey V. Khramchikhin Mariya A. Skrylnikova Iana L. Esaulkova Ekaterina O. Sinegubova Vladimir V. Zarubaev Maxim A. Gureev Aleksandra M. Puzyk Vladimir A. Ostrovskii 《Molecules (Basel, Switzerland)》2022,27(22)
This study of the interaction system of binucleophilic 3-substituted 4-amino-4H-1,2,4-triazole-5-thiols and 3-phenyl-2-propynal made it possible to develop a new approach to synthesis of such isomeric classes as 7-benzylidene-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine and 8-phenyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazepine. Among the 20 compounds studied in vitro against influenza A/Puerto Rico/8/34 (H1N1) virus, half of them demonstrated selectivity index (SI) of 10 or higher and one of them (4-((3-phenylprop-2-yn-1-yl)amino)-4H-1,2,4-triazole-3-thiol) possessed the highest (SI > 300). Docking results and values showed that the preferred interactant for our ligands was M2 proton channel of the influenza A virus. Protein-ligand interactions modeling showed that the aliphatic moiety of ligands could negatively regulate target activity level. 相似文献
15.
The mass spectrometric behaviour of four cis- and trans-la, 3-disubstituted -1,1 -dichloro-4-formyl-1a,2,3,4-tetrahydro-1H-azirino[1, 2-a] [1,5] benzodiazepines has been studied with the aid of mass-analysed ion kinetic energy spectrometry and exact mass measurements under electron impact ioniza-tion. All compounds show a tendency to eliminate a chlorine atom from the aziridine ring, and then eliminate a neutral propene or styrene from the diazepine ring to yield azirino[ 1, 2-6][1,3]benzimidazole ions. These azmno[1,2-a] [1,5]-benzodiazepines can also eliminate HCl, or Cl plus HG simultaneously to undergo a ring enlargement rearrangement to yield 1,6-benzodiazocine ions, which further lose small molecular fragments, propyne or phenylacetylene, with rearrangement to give quinoxaline ions. 相似文献
16.
以4-哌啶酮为原料,经过胺基保护、缩合、环合、脱保护等步骤,设计合成了一系列新型的5,6,7,8-四氢咪唑并[2',1':2-3]噻吩并[5,4-c]哌啶类化合物。通过核磁共振波谱仪(~1H NMR、~(13)C NMR)、质谱(MS)和元素分析确证了其结构。对其体外活性研究发现,该类化合物对乳腺癌细胞MCF-7具有一定的抑制活性,其中化合物5a的抑制活性最为显著,半数抑制浓度(IC_(50))值达到了8.6μmol/L。为此类化合物的抗肿瘤活性研究提供了参考。 相似文献
17.
2,7,16,21-四氧[8.8]对环吩-1,8,15,22-四酮是一个新的大环化合物。由于它的苯环不能自由转动,而苯环上的质子是化学位移不等价的。这给研究羰基的屏蔽和去屏蔽区域提供了一个很好的例证。 相似文献
18.
以4-氯-2-甲硫基-6-丙炔氧基嘧啶为原料,依次经Williamson醚合成、氧化和聚合反应制得新型四氧杂杯[2]芳烃[2]嘧啶母体(4),并通过点击化学反应合成了4个结构新颖的含1,2,3-三氮唑基团的四氧杂杯[2]芳烃[2]嘧啶衍生物(5a^5d),其结构经1H MNR,13C MNR和HR-MS(ESI)表征。采用MTT法研究了5a^5d对人宫颈癌细胞(Hela),人乳腺癌细胞(MCF-7),人肝癌细胞(HepG2)和人肺癌细胞(A549)的体外抗肿瘤活性。结果表明:化合物5a对MCF-7具有明显的抑制活性,在50μM浓度下抑制率可达82%,优于阳性对照药5-氟尿嘧啶。 相似文献
19.
In this study, we reported the synthesis of three kinds of mono-functional pillar[5]arene derivatives PRI, PRII and R and their structures were studied by 1D and 2D NMR spectra and mass spectra. The 2D NMR spectra including 1H-13C HSQC, 1H-1H COSY and NOESY spectra indicated that PRI and PRII are both stable self-included pseudo[1]rotaxanes in CDCl3. These original structures are promising compounds for the design of pillar[5]-based [1]rotaxane. And the results showed that R could exist stable in CDCl3 and DMSO because of the coordination of N-H?O hydrogen bonding interaction and C-H?π interaction. 相似文献
20.
A. M. El Massry 《Phosphorus, sulfur, and silicon and the related elements》2013,188(5):1143-1155
Reaction of phenylpyruvic acid with semicarbazide afforded 6-benzyl-2H-[1,2,4]triazine-3,5-dione ( 1 ) which upon oxidation with potassium dichromate furnished 6-benzoyl-2H-[1,2,4]triazine-3,5-dione ( 2 ) in good yield. Constructing pyrazolo[3,4-e][1,2,4]triazine system ( 4 ) was achieved by reacting 2 with arylhydrazines in ethanolic solution. However treatment of 2 with the less reactive heteroarylhydrazines gave only the corresponding hydrazones ( 3 ). Attempt for constructing 1,2,4,5,10-pentaaza-dibenzo[a,d]cyclohept-3-one ( 7 ) from 2 was failed and (benzoimidazol-2-yl) [1,2,4] triazine derivative ( 6 ) was the only product. Reaction of 1 with phosphorus pentasulphide afforded compounds 8 and 9 . Compound 8 was transformed to the hydrazino compound 14 , which led to the construction of triazolo[4,3-d] [1,2,4]triazine system. Thus compounds 15 and 16 were obtained by reacting 14 with carbon disulfide or acetic anhydride respectively. Attempt to couple 8 with chloroacetic acid failed, while it's known isomer 10 led to the formation of thiazolo [2,3-c] [1,2,4]triazine derivative ( 13 ). Simple theoretical calculation using AM1 and PM3 semiempirical Hamitonian provided rational ways to correlate the reactivity with structure proposed. 相似文献