α‐Cyanodithioic Acids and Their Corresponding Mono‐ and Dithiolate Salts as Building Blocks for the Synthesis of Novel Mercaptothiophenes

A novel and efficient method for the synthesis of mercaptothiophenes using cyanodithioic acids and their corresponding mono‐ and dithiolate salts as starting components is described.     

Sonochemical Synthesis of 1,4‐Disubstituted 1,2,3‐Triazoles in Aqueous Medium

An ultrasound‐accelerated fast and efficient three‐component reaction for the regioselective synthesis of l,4‐disubstituted 1,2,3‐triazoles using different alkyl and allyl halides, terminal alkynes, and sodium azide in water at room temperature has been developed using CuI as catalyst. Ultrasonication dramatically decreases the reaction times.     

Simple and Convenient Synthesis of 21‐Thioalkylether Derivatives of Methyl 16‐Prednisolone Carboxylates

The antedrug approach for corticosteroids has been described as a fundamentally sound approach for the development of safer anti‐inflammatory and anti‐asthmatic therapy. However, the derivatization of prednisolone and its congeners have been considered to be major pitfalls, because their syntheses are complicated by the presence of numerous carboxylate esters and hydroxyl functions in the steroid nucleus. A simple and direct synthesis of 21‐thioalkylether derivatives of methyl 16‐prednisolonecarboxylates is described. The 21‐mesylate of the methyl 16‐prednisolonecarboxylate and 9‐fluoro‐17‐dehydro methyl 16‐prednisolonecarboxylate were reacted with Na‐thioalkoxides to furnish the desired thioethers in good yields. A previously published method for the methanolysis of 16‐cyanoprednisolone to methylcarboxylate has been reexamined, and the conditions are explained clearly. The reaction conditions for all these reactions were critical.     

New Synthesis of 2‐Polyfluoroalkyl Substituted 1,4,5,6‐Tetrahydro‐pyrimidines and 4,5,6,7‐Tetrahydro‐1H‐1,3‐diazepines

A new efficient method for the preparation of 2‐polyfluoroalkyl substituted 1,4,5,6‐tetrahydropyrimidines and 4,5,6,7‐tetrahydro‐1H‐1,3‐diazepines by the reaction of polyfluoroalkanethiocarboxylic acids amides and 1,3‐propylenediamine or 1,4‐buthylenediamine is presented.     

Efficient Green Procedure for the Synthesis of Coumarin Derivatives by a One‐Pot,Three‐Component Reaction under Solvent‐Free Conditions

A simple, efficient, and general method has been developed for the synthesis of coumarin derivatives through a one‐pot reaction of aromatic aldehydes, 2,2‐dimethyl‐1,3‐dioxane‐4,6‐dione and 5,5‐dimethyl‐1,3‐cyclohexanedione, in the presence of TEBA under solvent‐free conditions using grinding methods. The mild reaction conditions, simple protocol, high yields, and cleaner reaction make this protocol practical and economically attractive.     

Selective Benzylic Bromination of 2-Methylnaphthalene

A practical synthesis of 2-(bromomethyl)naphthalene (1), by selective benzylic bromination of 2-methylnaphthalene (2), with bromine in heptane in the presence of lanthanum acetate hydrate is described.     

Oxidative Addition of 4-Hydroxycoumarin to Alkenes. An Expeditious Entry to 2,3-Dihydro-4H-furo-[3,2-c][1]benzopyran-4-ones1

In the presence of one-electron metal oxidants (CAN, MAH), 4-hydroxycoumarin (1) adds to alkenes to give 2,3-dihydro-4H-furo[3,2-c][1]benzopyran-4-ones.     

Organocatalytic Conjugate Addition of Azide Ion to α,β‐Unsaturated Aldehydes

An efficient and simple amine‐catatalyzed azide conjugate addition to α,β‐unsaturated aldehydes has been developed. In the presence of a catalytic amount of tertiary amine with a 1:1 mixture of NaN₃ and 37% HCl in CH₂Cl₂, α,β‐unsaturated aldehydes provided β‐azido aldehydes, which could be transformed into 1,3‐amino alcohols.     

Diammonium Hydrogen Phosphate as a Neutral and Efficient Catalyst for Synthesis of 1,8‐Dioxo‐octahydroxanthene Derivatives in Aqueous Media

A new and efficient method to synthesize a 3,3,6,6,9‐aryl‐1,8‐dioxo‐octahydroxanthene derivative using diammonium hydrogen phosphate as catalyst was performed in water at room temperature in a short periods.     

A Solvent‐Free Procedure for Synthesis of N‐Sulfonylimines Using Microwave Irradiation Catalyzed by ZrO2/S2O8 2− Solid Superacid

Abstract

A solvent‐free synthesis of N‐sulfonylimines from aldehydes with sulfonamides is described using ZrO₂/S₂O₈ ^2? as catalyst under microwave irradiation. This method is fast and high yielding for a range of substrates.