Synthesis of some novel 2,6‐disubstituted pyridazin‐3‐ones as TMC120 analogues

Different analogues of TMC120 derived from pyridazin‐3(2H)‐one rings were synthesized by coupling of 3,6‐dichloropyridazine with arylacetonitriles, phenols and/or aniline derivative followed by hydrolysis and alkylation with different benzyl bromide derivatives.     

Progress in the chemistry of 4‐ thiazolidinones

This review article includes a recent development in the chemistry of 4‐thiazolidinones. Structure, basicity, synthetic aspects, reactions, and applications were also reported.     

Studies with enamines and azaenamines: A novel efficient route to 6‐amino‐1,4‐dihydropyridazines and their condensed derivatives

1‐Arylhydrazonopyruvaldehydes 1 react with α,β‐unsaturated nitriles 2 to yield 6‐amino‐1,4‐dihydropyridazines 4 that are converted into pyridazinones 5 via refluxing in an acetic acid/hydrochloric acid mixture and into the ethylidenemalononitrile derivatives 6 on reflux with malononitrile in ethanolic/piperidine solution.     

Efficient synthesis of 6‐aryl‐2‐chloronicotinic acids via pd catalyzed regioselective suzuki coupling of 2,6‐dichloronicotinic acid

A regioselective Suzuki coupling of 2,6‐dichloronicotinic acid with aryl boronic acids to synthesize 6‐aryl‐2‐chloronicotinic acids is described. Regioselectivity was achieved in aqueous dioxane using the routinely used catalyst Pd(PPh₃)₄.     

Synthesis and antimalarial activity of 7‐benzylamino‐1‐isoquinolinamines

Computer modelling suggests that 7‐benzylamino‐1‐isoquinolinamines should mediate antimalarial effects by a mechanism distinct from that employed by existing antimalarial drugs. A series of these compounds was prepared in seven synthetic steps, via reductive amination of 1,7‐isoquinolinediamine. In vitro efficacy testing of the novel compounds against Plasmodium falciparum revealed them to be potent antimalarial agents.     

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