Syntheses and Biological Activities of Octahydro-1H-cyclopenta[d]pyrimidine Derivatives

Various nitromethylene derivatives were synthesized regioselectively. Compounds 8a − f were obtained by the reaction of 1-((5-chloropyridin-2-yl)methyl)-2-(nitromethylene)-octahydro-1 H -cyclopenta[ d ]pyrimidine ( 3 ) with primary amines and formaldehyde. The synthesized compounds were identified by 1 H NMR, HRMS (EI), and IR, and preliminary bioassays indicated that most of them showed moderate insecticidal activities against Aphis craccivora . The relationship between hydrophobicity and biological activity was also discussed.