Heterocyclic chemistry persists as an interesting psychology these days. Most of the published work in organic chemistry involves at least one heterocyclic ring. Microwave irradiation technique was much more conducive to attaining better yield. It also facilitated in reducing the usage of organic solvents and the reaction time. Easy separation was an added advantage of this method. The UV, IR, 1H NMR, 13C NMR, and MS data confirmed the proposed structure of the synthesized compounds. All the synthesized compounds were screened to assess their antiinflammatory potential. Acute toxicity study results revealed the absence of toxic manifestations at a dose of 1000 mg/kg body weight. Thus, the compounds were considered safe. 1/10thth and 1/20th of the safer dose was selected for the in vivo antiinflammatory.The anti-inflammatory activity of the benzopyrimidin-4(3H)-one scaffold improved considerably because of the presence of dimethoxy groups at the 6th and 7th positions and by 4-fluorophenyl substitution at the 2nd position.