An efficient chemo- and regioselective three component synthesis of pyridazinones and phthalazinones using activated KSF

<正>The first three-component and regioselective synthesis of pyridazinones and phthalazinones from arenes,anhydrides and ArNHNH_2 in the presence of efficient recyclable heterogeneous catalyst,montmorillonite-KSF,in high yield and short reaction time is reported.     

An efficient one‐pot synthesis of 2‐benzylpyrroles and 3‐benzylindoles

One‐pot regioselective benzylation of pyrroles and indoles using zirconium tetrachloride is discussed. This has been achieved by in‐situ generation of di(1H‐pyrrol‐1‐yl)zirconium(IV) chloride and di(1H‐indol‐1‐yl)zirconium(IV) chloride. It was observed that benzylation reactions of these complexes using n‐BuLi occurred at C‐2 position for pyrrole and C‐3 for indole. Copyright © 2011 John Wiley & Sons, Ltd.     

An efficient one‐pot synthesis of 2‐aminopyrimidinomethylnaphtols under solvent‐free conditions

A novel one‐pot three‐component condensation reaction of an aldehyde, 2‐aminopyrimidine and 2‐naphthol to afford the corresponding 2‐aminopyrimidinomethylnaphtols in good yields. The remarkable features of this new procedure are high conversions, short reaction time, clean reaction profiles, and environmentally benign and simple work‐up procedures.     

An efficient one‐pot synthesis of a new heterocyclic system with high‐fluorescent properties

Nucleophilic substitution of hydrogen in nitro derivative of imidazo[1,2‐a]pyridine has been used as a key step in the one‐pot synthesis of a new highly fluorescent heterocyclic system pyrido [1″,2″:1′,2′]imidazo[4′,5′:5,6]pyrido[2,3‐b]indole. J. Heterocyclic Chem., (2012).     

An efficient one‐pot synthesis of novel pyrimidoquinoline derivatives under microwave irradiation without catalyst

A series of pyrimidoquinoline derivatives were synthesized through one‐pot condensation of 2,6‐diaminopyrimidin‐4‐one, aldehyde and cyclic a 1,3‐dicarbonyl compound in glycol under microwave irradiation without catalyst. The protocol in the absence of catalyst has the advantage of good yield (87‐95%), short reaction time (4‐7 min) and an environmentally friendly technique.     

An expeditious one‐pot synthesis of substituted phenylazetidin‐2‐ones in the presence of zeolite

In this study, one‐pot rapid and efficient series of phenylazetidin‐2‐ones were synthesized from N,N‐dimethylaminobenzaldehyde, different substituted aromatic amines and phenylacetyl chloride in the presence of zeolite catalyst under microwave irradiation. We also reported schiff bases (1a–j) by classical and conventional microwave technique. The titled compounds are evaluated for their antimicrobial properties. The activities are due to C?O, C? N, linkages in 2‐azetidinones. All the compounds have shown comparable antibacterial activities. J. Heterocyclic Chem., (2011).     

An efficient one‐pot synthesis of diarylpyrazolo[1,5‐a]pyrimidine from isoflavones

Direct synthetic methods of 6,7‐diphenylpyrazolo[1,5‐a]pyrimidine derivatives have been developed. Cyclocondensation of isoflavones with 3‐aminopyrazole in the presence of sodium methoxide as alkali promoter gave 6,7‐diphenylpyrazolo[1,5‐a]pyrimidines in moderate to good yields. J. Heterocyclic Chem., (2011).     

An efficient one‐pot synthesis of n‐carboxymethylacridine‐1,8‐dione derivatives under microwave irradiation

A series of N‐carboxymethylacridine‐1,8‐dione derivatives were synthesized by one‐pot reaction of aldehyde, dimedone and glycine in glycol under microwave irradiation without catalyst with excellent yields (78‐92%) and short reaction time (4‐8min). And the reaction was not only suitable for aromatic monoaldehyde, but also aromatic dialdehyde.     

An efficient one‐pot synthesis of polyhydrobenzoacridine‐1‐one derivatives under microwave irradiation without catalyst

A series of 3,3‐dimethyl‐9‐substituted‐1,2,3,4,9,10‐hexahydrobenzo[c] acridine‐1‐ones and 3,3‐dimethyl‐9‐substituted‐1,2,3,4,9,10‐hexahydrobenzo[a] acridine‐1‐ones were synthesized by the reaction of an aldehyde, α‐naphthylamine or β‐naphthylamine and dimedone under microwave irradiation with short times and high yields.     

Microwave‐assisted one‐pot synthesis of functionalized pyrimidines using ionic liquid

An efficient one‐pot multicomponent synthesis of 2,4‐diamino‐5‐pyrimidinecarbonitrile derivatives has been achieved in excellent yields by the condensation of aromatic aldehydes, malononitrile, and guanidine using ionic liquid under controlled microwave irradiation (100 W) at 60°C. This green approach offers a number of advantages in terms of methodology, high‐product yield, short reaction time, mild reaction conditions, and easy workup. J. Heterocyclic Chem., (2011).     

An efficient one‐pot synthesis of dispiropyrrolidine derivatives through 1,3‐dipolar cycloaddition reactions under ultrasound irradiation

A series of dispiropyrrolidine derivatives were synthesized via the three‐component 1,3‐dipolar cycloaddition reaction of isatin, sarcosine and 5‐arylidene‐1,3‐thiazolidine‐2,4‐dione or 5‐arylidene‐4‐thioxo‐1,3‐thiazolidine‐2‐one in ethanol under ultrasound irradiation. This protocol has the advantages of mild reaction conditions, higher yields, and shorter reaction time. J. Heterocyclic Chem., (2011).     

An efficient one‐pot synthesis of pyrazolo[3,4‐b]pyridinone derivatives catalyzed by L‐proline

A series of 3‐methyl‐1,4‐disubstituted‐4,5‐dihydro‐1H‐pyrazolo[3,4‐b]pyridine‐6(7H)‐ones was synthesized via the three‐component reaction of aldehyde, 3‐methyl‐1‐phenyl‐1H‐pyrazol‐5‐amine, and Meldrum's acid catalyzed by L ‐proline. This protocol has the advantages of easier work‐up, milder reaction conditions, and high yields. J. Heterocyclic Chem., (2011).     

Solvent‐free one‐pot synthesis of pyrane derivatives

A straightforward and an efficient method for the synthesis of 2H‐pyrans via the one‐pot, reaction of alkyl bromides, carbon disulfide, secondary amines, activated acetylenes and isocyanides under solvent‐free conditions without using any catalyst at room temperature is reported. The method offers several advantages including high yields of products and an easy work‐up procedure. J. Heterocyclic Chem., (2011).     

An efficient one‐pot three‐component reaction for synthesis of spirooxindole derivatives in water media under catalyst‐free condition

An efficient, clean, and environmentally benign synthesis of spirooxindole derivatives by one‐pot three‐component reaction of isatins, malononitrile, and carbonyl compound in the absence of catalysis in water was described. A variety of spirooxindole derivatives were obtained with excellent yields within short reaction time. This novel protocol has the advantages of convenient operation, low cost, and environmental benign. © 2011 Wiley Periodicals, Inc. Heteroatom Chem 22:673–677, 2011; View this article online at wileyonlinelibrary.com . DOI 10.1002/hc.20723     

A convenient one‐pot synthesis of 1,2‐azaphospholanium salts

A novel facile one‐pot synthesis of the 1,2‐azaphospholanes by intramolecular alkylation of 3‐halopropyl amides of tricoordinate phosphorus has been suggested. Using this method, a series of the differently N‐substituted 1,2‐azaphospholanium salts were synthesized. 3‐Aminopropylphosphine oxides were obtained by hydrolysis of the salts. A probable mechanism of the 1,2‐azaphospholanium salts formation is discussed. © 2003 Wiley Periodicals, Inc. Heteroatom Chem 14:596–602, 2003; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.10209