One‐Pot Substitution‐Rearrangement Reaction of 2‐Chloroglycidic Ester: Effective Protocol for the Preparation of 3‐Arylsulfenyl‐2‐keto Ester

The one‐pot substitution‐rearrangement reaction of 2‐chloroglycidic ester is reported. Treatment of 2‐chloroglycidic ester with sodium arylthiolate at room temperature results in the formation of 3‐arylsulfenyl‐2‐keto ester in excellent to good yields.     

A Practical One‐Pot Synthesis of New S‐Glycosyl Amino Acid Building Blocks for Combinatorial Neoglycopeptide Synthesis

S‐Glycosyl L‐aspartic acid building blocks were synthesized starting from 1‐thiosugars by reaction with 5‐aminopentanol and suitably protected L‐aspartic acid pentafluorophenyl ester in a one‐pot procedure under Mitsunobu conditions using 1,1′‐azodicarbonyl dipiperidine and trimethyl phosphine. The method allowed for the preparation of S‐glycosyl amino acid building blocks in one step without protection of the amino function for the Mitsunobu condensation. Alternatively, the title compounds were prepared by a stepwise approach via 5‐aminopentyl 1‐thioglycosides.     

Rapid One‐Pot Preparation of 2‐Substituted Benzimidazoles from Esters using Microwave Conditions

A high‐yielding one‐pot procedure for the generation of 2‐substituted benzimidazoles first from esters using a microwave procedure is described.     

New One‐Pot Procedure for the Synthesis of 2‐Substituted Benzimidazoles

A highly selective synthesis of 2‐substituted benzimidazole derivatives from the reaction of o‐phenylendiamine derivatives and aromatic aldehydes in the presence of an organic salt, NH₄OAc, in absolute ethanol is presented. The products were obtained by evaporating the solvent followed by a simple recrystallization with excellent yields.     

One‐Pot Synthesis of Benzimidazoles from o‐Nitroanilines under Microwaves via a Reductive Cyclization

An efficient microwave irradiation synthesis of 2‐substituted benzimidazoles in one step via the Na₂S₂O₄ reduction of o‐nitroanilines in the presence of aldehydes is described. The method is simple and a good option to obtain the title compounds in a very short time.     

Convenient One‐Pot Heterogeneous Catalytic Method for the Preparation of 3,4‐Dihydropyrimidin‐2(1H)‐ones

A new, simple, environmentally friendly synthesis of dihydropyrimidinones from aromatic and aliphatic aldehydes, ethyl acetoacetate, and urea or thiourea using a small‐pore‐size zeolite as catalyst is described. Compared with the classical Biginelli reaction conditions, this method has the advantage of high yield, shorter reaction time, and recyclable and reusable catalyst.     

A Convenient One‐Pot Preparation of Stable Equivalents of Cyclobutane‐1,2‐dione and Cyclobutanetrione

A very short, high‐yielding, one‐pot procedure has been developed for the preparation of half‐protected cyclobutane‐1,2‐dione. This compound is much more stable than cyclobutane‐1,2‐dione itself and allowed further transformation to give diprotected cyclobutanetrione equivalents.     

One‐Pot Solvent‐Free Preparation of 2‐Phenyl‐1,3,2‐aryldioxaborins on Acidic Alumina

One‐pot, solvent‐free, microwave‐promoted preparation of 1,3,2‐aryldioxaborines on the surface of acidic alumina is described.     

Facile and Efficient One‐Pot Protocol for the Synthesis of Benzoxazole and Benzothiazole Derivatives using Molecular Iodine as Catalyst

Rapid and efficient condensation reactions of 2‐aminothiophenol and 2‐aminophenol with various aldehydes were carried out using I₂ in solvent‐free conditions with or without microwave irradiation to afford the corresponding 2‐substituted benzothiazole and benzoxazole derivatives in good to excellent yields.     

One‐Pot Synthesis of α‐Formyloxy Ketones from Enolizable Ketones

One‐pot synthesis of α‐formyloxy tones as well as α‐acetoxy ketones from enolizable ketones and [hydroxy(tosyloxy) iodo] benzene (HTIB)/polymer supported [hydroxy(tosyloxy) iodo] benzene (PSHTIB) in N,N–dimethylformamide (DMF)/N, N–dimethylacetamide (DMA) in high yields is described.     

Practical One‐Pot Procedure for the Synthesis of 1,2,3,4‐Tetrahydroquinolines by the Imino‐Diels‐Alder Reaction

A novel‐one‐pot procedure for the synthesis of tetrahydroquinolines via the imino‐Diels‐Alder reaction is described. This procedure gives better yields and exhibits better versatility for alkene substrates than the existing hemi‐aminal based methodologies.     

Microwave‐Assisted One‐Pot Preparation of Tetrahydro‐β‐carboline Hydrochlorides under Solvent‐Free Conditions

An efficient and environmentally friendly synthesis of tetrahydro‐β‐carboline hydrochlorides via Pictet–Spengler reaction was described. Tryptamine hydrochlorides were used as the reactant and no additional acid catalyst was needed. This reaction was completed within 2.5–9 min in good yield.     

One‐Pot Synthesis of Ene‐Lactams via N‐Debenzylation of Keto‐Containing N‐2,4‐Dimethoxylbenzylamides

Abstract

A general method of ene‐lactam preparation is described. Ene‐lactams can be prepared efficiently from keto‐containing N‐2,4‐dimethoxylbenzylamides in good to excellent yields. This method is applicable for the preparation of substituted δ‐, γ‐, and ?‐ene‐lactams and bicyclic ene‐lactams.     

Convenient One‐Pot Synthesis of Vinyl Ethers from Phenyl 2‐Hydroxyalkyl Selenides

Vinyl ethers were prepared with good yields in a one‐pot, two‐step transformation by O‐alkylation reaction of phenyl 2‐hydroxyalkyl selenides with primary or secondary organic halides followed by oxidation elimination with 30% hydrogen peroxide.     

Convenient One‐Pot Synthesis of Sulfonamides from Thiols using Trichloroisocyanuric Acid

A convenient synthesis of sulfonamides from thiols is described. In situ preparation of sulfonyl chlorides from thiols is accomplished by oxidation with trichloroisocyanuric acid (TCCA), benzyltrimethylammonium chloride and water (2.5 equiv). The sulfonyl chlorides are then further allowed to react with excess amine in the same reaction vessel. Triethylamine can be optionally added as acid scavenger.     

Facile One‐Pot Synthesis of Oxazolidin‐2‐ones from Phenyl 2‐Hydroxyalkyl Selenides

A novel, convenient, efficient, three‐step, one‐pot synthesis of 2‐oxazolidinones from phenyl 2‐hydroxyalkyl selenides was developed. Using this methodology, 2‐oxazolidinones are obtained in good yields (76–85%) by reaction of phenyl 2‐hydroxyalkyl selenides with benzoyl isocyanate and subsequent oxidation/cyclization, followed by hydrolysis with hydrochloric acid solution.     

One‐Pot Preparation of Unsymmetrical Biaryls via Suzuki Cross‐Coupling Reaction of Aryl Halide using Phase‐Transfer Catalyst in a Biphasic Solvent System

A one‐pot synthetic method of unsymmetrical biaryls was developed via the Suzuki cross‐coupling reaction of aryl halide using a phase‐transfer catalyst in a biphasic solvent system.     

Simple,One‐Pot Procedure for the Generation of Homoallylic Alcohols from Barbier‐Type Allylation of Gem‐diacetates in the Presence of β‐Cyclodextrin in Water

A novel and highly efficient allylation of gem‐diacetates using allylbromide has been developed in aqueous medium catalyzed by β‐cyclodextrin in the presence of Zn‐mediated Barbier‐type allylation to afford the corresponding homoallylic alcohols in good yields. The β‐cyclodextrin can be recovered and reused for a number of runs without significant loss of activity.     

One‐Pot Preparation of Fluorinated α‐Aminoalkyl Phosphonates under Microwave Irradiation and Solvent‐Free Conditions

A facile one‐pot method has been developed for the synthesis of fluorine‐containing α‐amino phosphonates in good yields by a three‐component reaction of fluorinated aromatic aldehydes, anilines, and diethyl phosphate in the presence of a silica‐gel support under microwave irradiation within 10 min. All new compounds are fully characterized by spectral methods and elemental analysis.     

Convenient One‐Pot Procedures for the Synthesis of 2,2′:6′,2″‐Terpyridine

One‐pot reactions to produce 2,2′:6′,2″‐terpyridine (tpy) under mild conditions are described under both solventless and solvent‐assisted conditions. Tpy can be obtained in 32% yield in a simple one‐pot reaction, which can readily be scaled‐up to give large quantities of tpy. These new approaches are superior to those previously described because of the fast and efficient synthesis and purification of tpy.