A Convenient One-Pot Synthesis and Nematicidal Activity of Nicotinic Acid Amides

Russian Journal of Organic Chemistry - Seven nicotinic acid amides were synthesized by condensation of nicotinic acid adsorbed on silica gel with different aromatic amines. The synthesized...     

One-Pot Synthesis of N-2,4-Enyne Cyclic Amines

Russian Journal of General Chemistry - Stereoselective synthesis of N-2,4-enyne cyclic amines was performed by one-pot animation of individual isomers of 1,3-dichloropropene and the subsequent...     

A Facile One-Pot Transformation of Carboxylic Acids to Amides

Carboxylic acids, converted in situ into carboxylic-(p-nitrobenzene)sulfonic anhydrides using p-nitrobenzenesulfonyl chloride, Et3N, and DMAP in CH₃CN, react with primary or secondary amines, to give amides in high yields.     

新型酰胺类化合物的合成及其生物活性

选取原儿茶酸和胡椒酸两种羧酸化合物,通过酰胺键与L-酪氨酸甲酯、D-酪氨酸甲酯、章胺、多巴胺4种具有生物活性的胺类的化合物偶联。成功合成了8个新型酰胺类化合物,其结构经¹H NMR和 ¹³C NMR表征。此外,还测试所有目标分子的体外酪氨酸酶抑制活性和DPPH自由基清除能力,对目标分子的酪氨酸酶抑制活性和抗氧化活性进行了初步评价。      

Facile One-Pot Conversion of Aldehydes into Amides

A facile one-pot synthesis of amides from aldehydes has been developed. This tandem process involves the formation of a nitrile intermediate obtained from the reaction of an aldehyde with hydroxylamine hydrochloride in dimethylsulfoxide at 100°C and the subsequent treatment of the nitrile with basic hydrogen peroxide. The resulting amide products were produced in good yields (67–95%) and purity (>95%).     

A Novel One-Pot Synthesis of Fluorinated α,β-Unsaturated Esters

The reaction of pentafluorophenylmethylene-triphenylarsorane or p-chloro-tetrafluorophenylmethyl-enetriphenylarsorane, generated in situ from methylene-triphenylarsorane and hexafluorobenzene or chloropenta-fluorobenzene, with bromoacetates giving excellent yields of 3-pentafluorophenyl or 3-p-chloro-tetrafluoro-phenyl α, β-unsaturated esters with high steroselectivity is described.     

A Novel One-Pot Synthesis Ofesters Byexchange Reactions between Carbonates and Anhydrides

A new method for the synthesis of esters by exchange reaction between anhydrides and carbonates, without any solvent, in the presence of Ti or Sn based catalyst is presented.     

Novel Synthesis of N-Substituted p-Hydroxybenzoic Amides on Soluble Polymer-Support

The synthesis of N-substituted p-hydroxybenzoic amides using a liquid phase approach is described. Poly(ethylene glycol)(PEG) and p-hydroxybenzoic acid were linked by oxalyl chloride to give compound 1, which was chlorinated by thionyl chloride, followed by amidation with NHR^1R^2 to yield compound 3. Hydrolysis of compound 3 gave the title amide 4.These crude library members were obtained in good yields with high purities.     

Novel One-Pot Synthesis of Tetrasubstituted Phenolic Ketones and Sulphones

Reaction of tetrasubstituted cyclopentadienones 1,1a with phenacyl bromide 2, dichloroacetophenone 3, ethyl bromomalonate 4, bromomethyl-p-tolylsulphone 5 in 50% NaOH and in the presence of benzyltriethylammonium chloride gave the carbene adduct 6,7,7a as well as pentasubstituted phenols 8,9,9a,10,10a,11,11a. The carbene adducts 6,7 and 7a were also converted into the phenols 8,9,9a using t-BuOK or NaOH in refluxing t-BuOH.     

Novel One-Pot Procedure for the Synthesis of 1,2-Diketones

A simple and convenient one-pot procedure is reported for the synthesis of 1,2-diketones from corresponding benzoin-type condensation reaction of aromatic aldehydes in water with N,N-dialkylbenzimidazolium salt as condensation catalyst and ferric chloride as oxidizing reagent.     

Phase Transfer Catalyzed Synthesis of Amides and Esters of 2,4-Dichlorophenoxyacetic Acid

A convenient procedure is reported for the preparation of amides and esters via the reaction of 2,4-dichlorophenoxyacetyl chloride with amines or phenols under the condition of liquid-liquid phase transfer catalysis using polyethylene gtycol-600 as the catalyst. The products have been characterised on the basis of analytical and spectral (IR and H-NMR) data.     

三组分一锅法合成新型三唑及双三唑类化合物

以氰化亚铜作为催化剂,以乙酰氧基丙烯酸酯衍生物、叠氮化钠和取代的芳炔为原料,在水中一锅法合成新型1,4-二取代-1,2,3-三唑和双三唑化合物,该方法具有操作简单、不需要碱和收率高的优点.     

One-Pot Route from Halogenated Amides to Piperidines and Pyrrolidines

Piperidine and pyrrolidine derivatives are important nitrogen heterocyclic structures with a wide range of biological activities. However, reported methods for their construction often face problems of requiring the use of expensive metal catalysts, highly toxic reaction reagents or hazardous reaction conditions. Herein, an efficient route from halogenated amides to piperidines and pyrrolidines was disclosed. In this method, amide activation, reduction of nitrile ions, and intramolecular nucleophilic substitution were integrated in a one-pot reaction. The reaction conditions were mild and no metal catalysts were used. The synthesis of a variety of N-substituted and some C-substituted piperidines and pyrrolidines became convenient, and good yields were obtained.     

Novel One-Pot Synthesis of New Oxindole Derivatives Catalyzed by PTSA

The one-pot synthesis of spirooxindoles via three-component reaction of urea, isatin, and 1,3-dicarbonyl compounds in the presence of a catalytic amount of p-toluenesulfonic acid in acetonitrile has been carried out.

One-Pot Synthesis of Novel Rhodanine Based Ketenimines Via Multicomponent Reactions

Abstract

Synthesis of polyfunctionalized ketenimines via three-component reactions of rhodanine and 5-(4-dimethylaminobenzylidene)-rhodanine with dialkyl acetylenedicarboxylates and alkyl isocyanides is described. The reactions proceed smoothly under mild conditions leading to the desired products in good yields. In the case of methyl acetylenecarboxylate, the reaction led to methyl (Z)-3-({5-[(E)-1-(tert-butylamino)methylidene]-4-oxo-4,5-dihydro-1,3-thiazol-2-yl}sulfanyl)-2-propenoate in low yield.

GRAPHICAL ABSTRACT      

A Facile One-Pot Synthesis of Vinpocetine

A one-pot synthesis of vinpocetine from vincamine was established. Lewis acids caused transesterification and/or dehydration of vincamine in EtOH. FeCl₃ catalyzed both transesterification and dehydration while Ti(OEt)₄ selectively catalyzed transesterification.     

One-Pot synthesis of unsymmetrically substituted 2,4-dialkylisoflavenes

The trimethylsilyl derivative of formonometine reacts sequentially with two different organometallic derivatives to afford regiospecifically and with good yield 2,4-dialkylisoflavenes unsymmetrically substituted.     

A One-Pot Approach to Novel Pyridazine C-Nucleosides

The synthesis of glycosides and modified nucleosides represents a wide research field in organic chemistry. The classical methodology is based on coupling reactions between a glycosyl donor and an acceptor. An alternative strategy for new C-nucleosides is used in this approach, which consists of modifying a pre-existent furyl aglycone. This approach is applied to obtain novel pyridazine C-nucleosides starting with 2- and 3-(ribofuranosyl)furans. It is based on singlet oxygen [4+2] cycloaddition followed by reduction and hydrazine cyclization under neutral conditions. The mild three-step one-pot procedure leads stereoselectively to novel pyridazine C-nucleosides of pharmacological interest. The use of acetyls as protecting groups provides an elegant direct route to a deprotected new pyridazine C-nucleoside.