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1.
This paper describes an efficient approach for the synthesis of 2‐(trifluoromethyl)‐1,2,3,4,7,8‐hexahydroquinolin‐5(6H)‐one derivatives via a one‐pot four‐component reaction of aromatic aldehyde, 5,5‐dimethylcyclohexane‐1,3‐dione, 4,4,4‐trifluoro‐1‐(thien‐2‐yl)butane‐1,3‐dione, and NH4OAc with excellent yields at room temperature. In this synthesis, the trifluoromethyl was efficiently introduced in hexahydroquinoline structure, and they may be valuable the drug candidates. This approach also offered several other advantages, such as catalyst‐free, mild conditions, and simple experimental operation.  相似文献   

2.
Strategies to address mounting environmental concerns with current approaches include an operationally simple and highly efficient one‐pot three‐component approach for the synthesis of spiro[imidazo[2,1‐b][1,3]oxazine‐7,3′‐indoline derivatives, which has been developed via Huisgen zwitter ion intermediate. The significant advantages of this protocol are short reaction time, excellent yields, and facile formation of three new bonds in one operation from easily available starting materials.  相似文献   

3.
An unexpected FeCl3‐mediated three‐component cascade reaction has been used to construct structurally diverse pyrrolo[1,2‐c]quinazolinone derivatives with potential biological activities. This method has advantages of mild conditions, simple work‐up, as well as wide substrate scope, which makes it a powerful approach to the synthesis of diverse pyrrolo[1,2‐c]quinazolinones. This cascade reaction involves 1,3‐dipolar cycloaddition between azomethine ylides and allenoates, followed by intramolecular nucleophilic addition in the presence of FeCl3. The obtained products could be easily transformed into derivatives with the pyrrolo[2,3‐c]quinazoline alkaloid skeleton.  相似文献   

4.
A simple and efficient one‐pot synthesis of alkyl‐2‐(alkylimino)‐4‐methyl‐3‐phenyl‐2,3‐dihydrothiazole‐5‐carboxylate and dialkyl 3,3′‐(1,4‐phenylene)‐bis‐[2‐(alkylimino)‐4‐methyl‐2,3‐dihydrothiazole‐5‐carboxylate] derivatives from the reaction of phenylisothiocyanate (and also 1,4‐phenylene diisothiocyanate) and primary alkylamines in the presence of 2‐chloro‐1,3‐dicarbonyl compounds is described. This new protocol has several advantages such as lack of necessity of the catalyst and solvent, good yields,mild conditions and short times for reaction.  相似文献   

5.
The synthesis of polyfunctionalized 7‐amino‐5‐(4‐aroyl)‐1,3‐dimethyl‐2,4‐dioxo‐1,2,3,4,5,8‐hexahydropyrido[2,3‐d ]pyrimidine‐6‐carbonitrile derivatives by a green approach was achieved via one‐pot three‐component reaction of arylglyoxals, malononitrile, and 1,3‐dimethyl‐6‐aminouracil in the presence of urea as organocatalyst in EtOH:H2O (1:1) at 60°C. This protocol provides a mild and fast procedure to structurally diverse bicyclic pyridopyrimidines in good to excellent yields.  相似文献   

6.
An efficient cascade process five‐component reaction of isatins and 3‐oxo‐N‐arylbutanamide for the synthesis of 4,4′‐((2‐oxoindoline‐3,3‐diyl)bis(methylene))bis(2‐aryl‐1H‐pyrrolo[3,4‐c]quinoline‐1,3(2H)‐dione) derivatives was reported under mild condition. The advantages of this strategy are easy to obtain raw materials, convenient one‐pot procedure, and simple operation.  相似文献   

7.
A new approach to the synthesis of new heterocyclic compounds with triazine and 4‐thiazolidone fragments in one molecule is developed. The synthesis methods comprise [2+3]‐cyclocondensation reactions essential in the preparative synthesis of 4‐thiazolidone derivatives. The reactions of S,N‐nucleophiles with C2‐cyclization agents for the synthesis of a number of biologically active 2‐triazin‐4‐thiazolidones were investigated. The interaction of thiosemicarbazone of sym‐triazine with derivatives of α‐halogencarboxylic acids and maleic anhydride resulted in correspondent (2‐[2‐(4,6‐dichloro‐1,3,5‐triazin‐2‐yl)hydrazino]‐5‐(3,4,5‐ R‐p‐phenyl‐methyliden)‐1,3‐thiazol‐4‐ones obtained in the one‐step synthesis. © 2010 Wiley Periodicals, Inc. Heteroatom Chem 21:392–396, 2010; View this article online at wileyonlinelibrary.com . DOI 10.1002/hc.20631  相似文献   

8.
An efficient solvent‐free one‐pot stereoselective synthesis of 4‐hydroxy‐1,3‐thiazinane‐2‐thione derivatives from the reaction of primary amines and carbon disulfide in the presence of α,β‐unsaturated aldehydes has been reported. The 4‐hydroxy‐1,3‐thiazinane‐2‐thione derivatives were easily converted to the related dehydrated or acetylated products.  相似文献   

9.
An efficiently synthesis of chromones via cyclodehydration of corresponding 1‐(2‐hydroxyphenyl)‐3‐(pyridine‐3‐yl)propane‐1,3‐dione is described under ultrasound irradiation. A series of novel 2‐(pyridine‐3‐yl)‐4H‐chromen‐4‐one derivatives was confirmed on the basis of 1H‐NMR, mass, IR spectral data, and elemental analysis. The synthesized compounds were evaluated for their antibacterial and antifungal activities. Most of the compounds were found to be comparable potent than the reference standard drugs. Utilization of ultrasound irradiation, simple reaction conditions, isolation, and purification makes this manipulation very interesting from an economic and environmental perspective.  相似文献   

10.
The present article reports our approach toward the synthesis of spiro compounds via indol‐2,3‐diones. Thus, reaction of indol‐2,3‐dione derivatives with a secondary cyclic amino acid, namely, (R)‐(−)‐thiazolidine‐4‐carboxylic acid, affords a thiazolo‐oxazolidinone as the main product. When the reaction is carried out in the presence of a dipolarophile, 1,3‐dipolar cycloaddition to the intermediate azomethine ylide leads to a novel spiro compound. The products have been characterized on the basis of spectral studies, and the geometry of the intermediate iminium compound has been optimized by use of the semiempirical molecular orbital method. © 1999 John Wiley & Sons, Inc. Heteroatom Chem 10: 381–384, 1999  相似文献   

11.
An efficient and green reactions of isatins, 3‐amine‐1H‐pyrazole (5‐methyl‐1H‐pyrazol‐3‐amine) and 1,3‐diketone in aqueous medium for the synthesis of novel 1′,7′,8′,9′‐tetrahydrospiro[indoline‐3,4′‐pyrazolo[3,4‐b]quinoline]‐2,5′(6′H)‐dione derivatives were reported in this research. The advantages of this reaction are simple operation, mild‐reaction conditions, wide scope substrate, high yields, and friendly environment. The products were confirmed by IR, 1H NMR, 13C NMR, and HRMS.  相似文献   

12.
An efficient approach for one‐pot synthesis of biologically active new spiro[chroman‐3,2′‐chromeno[2,3‐b ]furan]‐2,4,4′‐(3′H )‐trione derivatives from tandem Knoevenagel–Michel addition–heterocyclization reaction between 4‐hydroxycumarin and various aldehydes in the presence of N,N,N ,N ′‐tetrabromobenzene‐1,3‐disulfonamide as an efficient catalyst at ambient temperature under solvent‐free conditions was reported. Simple procedure, high yields, easy work‐up, and reusability of the catalyst are the significant advantages of this process.  相似文献   

13.
The new approach involving the solid supported catalyst for the formation of C–N bond followed by cyclization has been reported. In this work we have reported a facile, efficient, and environment‐friendly protocol for the synthesis of some new 3‐amino‐imidazo[2,1‐b](1,3)benzothiazole derivatives by one‐pot condensation of 2‐aminobenzothiazole, indole‐3‐carbaldehyde, and aryl isocyanide in the presence of silica‐supported P2O5 as a heterogeneous solid acid catalyst. The reaction was performed using conventional method under green conditions. The present approach offers the advantages of simple methodology, inexpensive acid catalyst, short reaction time, easy work up with excellent yield, simple purification and use of green solvent. All the newly synthesized compounds were characterized in details using physical and chemical techniques such as melting point, 1H NMR, 13C NMR, and FTIR spectroscopy.  相似文献   

14.
In this study, we developed a new protocol for the preparation of the chiral 3‐[(E)‐enoyl]‐1,3‐oxazolidin‐2‐ones under the ultimately simple reaction conditions starting with the corresponding enoyl chlorides and 1,3‐oxazolidin‐2‐ones with Et3N/LiCl at room temperature. The method generally allows efficient preparation of various derivatives regardless of the steric and electronic nature of the substituents on both the enoyl or the oxazolidinone sites. Excellent yields, combined with the simplicity of the experimental procedures, render the present method immediately useful for preparing the target compounds.  相似文献   

15.
A simple and efficient synthesis of 2‐amino‐4‐aryl thiazole derivatives was carried out through the reaction of substituted acetophenones and thiourea using three different types of catalytic systems including N,N,N′,N′‐tetrabromobenzene‐1,3‐disulfonamide [TBBDA], poly(N,N′‐dibromo‐N‐ethylbenzene‐1,3‐disulfonamide) [PBBS] and a combination of TBBDA and nano‐magnetic catalyst supported with functionalized 4‐amino‐pyridine silica (MNPs@SiO2‐Pr‐AP). The results showed that the use of TBBDA along with the MNPs@SiO2‐Pr‐AP gains the highest yields of the products in the shortest reaction time.  相似文献   

16.
An efficient one‐pot synthesis of 5‐(trifluoromethyl)‐4,7‐dihydro‐7‐aryl‐[1,2,4]triazolo[1,5‐a]pyrimidine derivatives was performed via the reaction of aryl aldehyde, 3‐amino‐1,2,4‐triazole and ethyl 4,4,4‐trifluoro‐3‐oxobutanoate or 4,4,4‐trifluoro‐1‐phenylbutane‐1,3‐dione in ionic liquid. This method has the advantages of short synthetic route, operational simplicities, mild reaction conditions, high yields and eco‐friendliness.  相似文献   

17.
3(2‐pyridinylmethylene)‐5‐aryl‐2(3H)‐furanones and 3(3‐pyridinylmethylene)‐5‐aryl‐2(3H)‐furanones were prepared as a mixture of (E) and (Z) stereoisomers by condensing pyridine‐2‐carboxaldehyde and pyridine‐3‐carboxaldehyde with 3‐aroylpropionic acids. The reaction of the furanones 6 and 7 with anhydrous aluminium chloride in benzene led to the formation of 4,4‐diaryl‐1‐(2‐pyridinyl)but‐1,3‐diene ( 8 ) and 4,4‐diaryl‐1‐(3‐pyridinyl)but‐1,3‐diene ( 9 ) as mixtures of geometrical (E,E‐ and E,Z‐) stereoisomers via an intermolecular alkylation mode. When the reaction was carried out in tetrachloroethane as a solvent, the reaction of 6 gave 5‐arylquinoline‐7‐carboxylic acid via intramolecular alkylation mode. This may be considered as a novel method for the synthesis of quinoline derivatives. J. Heterocyclic Chem., (2011).  相似文献   

18.
A three‐component system of one‐pot synthesis of [1,2,4]triazolo[1,5‐a]pyrimidine derivatives using condensation of 1,3‐dicarbonyl compounds, aldehydes, and 5‐amino[1,2,4]triazole in ethanol without any catalyst was reported in high yields via simple, efficient, and environmentally friendly process. The method reported herein considered a green process; this method has significant advantages of simple workup procedure, excellent yield, minimal environmental pollution, and short reaction time over classical reported methods.  相似文献   

19.
A simple and efficient one‐pot synthesis of alkyl 2‐(alkyl)‐4‐methyl‐2‐thioxo‐2,3‐dihydrothiazole‐5‐carboxylates from the reaction of primary alkylamines and carbon disulfide in the presence of 2‐chloro‐1,3‐dicarbonyl compounds is described. This new protocol has several advantages such as lack of necessity of the catalyst, good yields, mild conditions and short times for reaction.  相似文献   

20.
屠树江     朱晓彤     房芳     章晓镜     朱松磊     李团结     史达清  王香善     纪顺俊 《中国化学》2005,23(5):596-598
A simple effective synthesis of bis(dihydropyrimidinone-4-yl)benzene derivatives, using boric acid as catalyst,from isophthalic aldehyde or terephthalic aldehyde, 1,3-dicarbonyl compounds and urea or thiourea in glacial acetic acid was described. As the expansion of the classical Biginelli reaction, this method has the advantage of excellent yields 83%-94% and short reaction time 0.5-1.5 h.  相似文献   

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