An improved synthesis of 1‐acetyl‐1H‐indol‐3‐yl acetates

An efficient two steps procedure for the synthesis of 1‐acetyl‐1H‐indol‐3‐yl acetates, starting from 2‐chlorobenzoic acids, was developed and in general, moderate to good yields were obtained     

Synthesis of substituted amino‐cycloalkyl[b]thieno‐[3,2‐e]pyridines

An efficient two respectively three steps procedure for the synthesis of cycloalkyl[b]thieno[3,2‐e]‐pyridine amines was developed and in general good to very good yields were obtained.     

Synthesis of new terpolymers with heterocyclic pendant groups

Chemical modifications of polyacrylonitrile (PAN), an inexpensive and commercial homopolymer, to obtain terpolymers containing 1,2,4 or 1,3,4 oxadiazolic pendant groups are described. These new materials are physically and spectroscopically characterized.     

Synthesis of N‐benzoylamino‐1,2,3,6‐tetrahydropyridine derivatives as potential anti‐inflammatory agents

N‐Benzoylamino‐1,2,3,6‐tetrahydropyridines 9a‐q were synthesized from 4‐substituted pyridines in four steps. Amination of pyridines was carried out to prepare intermediate N‐aminopyridinium mesylates using mesytelenesulfonyl hydroxmate (MSH) as aminating agent. N‐aminopyridinium mestylates reacted with appropriately substituted acyl chlorides to form N‐ylides as stable crystalline solids. Partial reduction of N‐ylides with mild reducing agent afforded N‐benzoylamino‐1,2,3,6‐tetrahydropyridines in fair to good yields.     

Synthesis and herbicidal activities of a series of di(aminopyrazoly) ketone derivatives

In order to obtain new lead compounds with high herbicidal activity, a series of 5‐amino pyrazole derivatives were designed and synthesized using a series of relational synthons. Their structures were determined by IR, ¹H NMR, and elemental analyses. These compounds were screened for herbicidal activities against rape and barnyard grass. Their structure‐activity relationships are discussed.     

Traceless synthesis of quinazoline‐2,4‐diones by curtius rearrangement reaction using poly(ethylene glycol) as soluble polymeric support

We have developed an efficient method to synthesize various quinazoline‐2,4‐diones using poly‐(ethylene glycol) as soluble polymeric support. The procedure of this reaction included: formation of acyl azide, efficient Curtius rearrangement, nucleophlic addition with amines to produce ureas, cyclization and concurrent cleavage of the resulted six‐membered heterocycle from PEG‐support in excellent yields. This method is mild and manipulation is easy.     

Microwave solvent free regioselective 1,3 dipolar cycloaddition in the synthesis of 1,4 substituted [1,2,3]‐triazoles as amide bond isosteres

1,3 Dipolar cycloaddition of Fmoc‐amino azides and acetylenic amides produces under solvent free irradiation a mixture of 1,4 or 1,5 substituted [1,2,3]‐triazoles. The presence of copper (I) iodide, plays a central role on regioselectivity. Four Fmoc‐amino azides characterized by different steric hindrance in side chains, and three different terminal alkynes, provided only the 1,4 substituted regioisomer under thermal microwave heating. Good yields, low consumption of organic solvents and short reaction times are the main aspects of our procedure. Reactions are compared to regioselective copper (I) catalysed solution synthesis performed at room temperature.     

Microwave assisted synthesis of thiazolo[3,2‐b][1,2,4]‐triazoles containing 1,8‐naphthyridine moiety

A simple and efficient protocol for the synthesis of 5‐aryl‐2‐(2‐substituted‐1,8‐naphthyridin‐3‐yl)‐thiazolo[3,2‐b][1,2,4]triazoles ( 4 ) is achieved by cyclocondensation of 3‐(2‐substituted‐1,8‐naphthyridin‐3‐yl)‐1,2,4‐triazoles ( 3 ) with α‐halogenoketones in anhyd. methanol under microwave irradiation. The products are obtained in good yields and in a state of high purity.     

Synthesis of beta‐proline like derivatives and their evaluation as sodium channel blockers

A simple and convenient procedure for the preparation of beta‐proline like derivatives in their racemic and optically active forms has been reported. The compounds have been screened for their potential activity as sodium channel blockers.