Keywords
1 3-dielectrophiles
5-a]pyrimidine
aza-Michael addition
bis(aldehyde)
heterocyclization
in vitro antibacterial screening.
multicomponent reactions
pyrazolo[1
α-unsaturated nitriles
Abstract
A three-component protocol was adopted to efficiently prepare new bis(pyrazolo[1,5-a]pyrimidines) linked to different spacers in 80-92% yields from 1H-pyrazole-3,5-diamines, malononitrile and bis(aldehydes). The p-xylene-linked bis(pyrimidine) bearing 3-positioned 4-methoxy-benzyl substituent had the best antibacterial activity with MIC / MBC values up to 2.2 / 4.4 µm.
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