This paper reports a comparative study of the chemoselectivity and yields of the synthesis of N-alkyl-4-(trihalomethyl)-1H-pyrimidin-2-ones carried out by the cyclocondensation of 4-alkoxy-1,1,1-trihalo-3-alken-2-ones (enones) with methyland allylureas with the N-alkylation of 4-(trihalomethyl)-1H-pyrimidin-2-ones with methyl iodide and allyl bromide. To determine the chemoselectivity of the products obtained, all compounds were fully analyzed by 1 H and 13 C NMR and 2D HMBC spectroscopy. This study has demonstrated that the

Cinco derivados de 4-trifluorometil-2-(5-aril-3-stiril-1H-pirazol-1il)-pirimidinas e seis 5-aril-3-estiril-1-carboxamidino-1H-pirazois previamente sintetizados foram avaliados de acordo com suas propriedades antioxidantes e antimicrobianas. Estas atividades foram avaliadas por ensaios de DPPH e HRP/luminol/H 2 O 2 quimioluminescência e suas atividades antimicrobianas (CIM). Os resultados foram bons para alguns compostos da série em certas concentrações em comparação direta com padrões.Five previously synthesized 4-trifluoromethyl-2-(5-aryl-3-styryl-1H-pyrazol-1yl)-pyrimidines and six 5-aryl-3-styryl-1-carboxamidino-1H-pyrazole derivatives were screened for their antioxidant proprieties. The antioxidant activities were evaluated by using the DPPH and the HRP/luminol/H 2 O 2 chemiluminescence assay systems and for their antimicrobial activity (MIC). The results were good for those series in some concentration in comparison with the standards.

No abstract

S y n t h e s i s o f S o m e N o v e l P y r i m i d o [ 1 , 2 -a ] b e n z i m i d a z o l e sAbstract: The synthesis of some potentially active 2-(trifluoromethyl)pyrimido[1,2-a]benzimidazoles and pyrimido[1,2-a]benzimidazol-2(1H)-ones by the cyclization of 4-alkoxyvinyl trifluoro(chloro)methyl ketones with 2-aminobenzimidazole is described. The structure of the products was assigned based on 1 H and 13 C NMR as well as 2D-NMR experiments. Some of the obtained products exhibited significant DNA-topoisomerase I inhibitory activity.

Reaction of 4-trichloromethyl-1H-pyrimidin-2-ones with 5-bromo-1,1,1-trichloro(fluoro)-4-methoxy-alk-3-en-2-ones affords 1-[5,5,5-trichloro(fluoro)-2-methoxy-4-oxopent-2-en-1-yl]-4-trichloromethyl-1H-pyrimidin-2-ones. Reaction of the latter trichloromethylated compound with amines, hydroxylamine, and hydrazines affords a series of 1-(2-alkylamine-5,5,5-trichloro-4-oxopent-2-en-1-yl)-4-trichloromethyl-1H-pyrimidin-2-ones and 1-(5-trichloromethyl-5-hydroxy-4,5-dihydro-3-azol-3-ylmethyl)-4-trichloromethyl-1H-pyrimidin-2-ones, respectively.