A facile synthesis of 1‐alkyl‐5‐arylalkoxy‐6‐methoxy‐3,4‐dihydroisoquinolines

1‐Alkyl‐5‐arylalkoxy‐6‐methoxy‐3,4‐dihydroisoquinolines were synthesized by the alkylation of 1‐alkyl‐5‐hydroxy‐6‐methoxy‐3,4‐dihydroisoquinolines with arylalkyl halide in the presence of potassium carbonate. 1‐Alkyl‐5‐hydroxy‐6‐methoxy‐3,4‐dihydroisoquinolines as key precursor prepared from o‐vaniline via 6 steps.     

Synthesis and anti‐HIV‐1 evaluation of 1,5‐disubstituted pyrimidine‐2,4‐diones

1,5‐Disubstituted pyrimidine‐2,4‐diones were synthesized by fusion of 5‐bromouracil with an aniline derivative followed by coupling with benzyl halide whereas the opposite synthesis sequence failed. Also 4,6‐dichloro‐N,N,5‐trimethylpyrimidin‐2‐amine was treated with phenols. The products were tested for their activity against HIV‐1.     

Chemistry and application of 4‐oxo‐4H‐1‐benzopyran‐3‐carboxaldehyde

The Chemistry and application of the title aldehyde and some simple derivatives thereof are reviewed.     

Photocyclisations of some 3‐alkoxy‐2‐thienylchromones

Photoreorganisations of some 3‐allyloxy‐2‐thienylchromones have been described. The photoreactions are initiated through the intramolecular H‐abstraction to provide angular tetracyclic compounds. These chromones yield good chemical efficiency due to the involvement of highly stabilized allylic 1,4‐biradicals.     

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.