Synthesis and reactions of some biologically active 2-(2'-thienyl)benzoxazinone and quinazolinone derivatives

Pharmazie. 1989 May;44(5):312-5. doi: 10.1002/chin.198946210.

Abstract

Different amines were found to attack the hitherto unknown 6,8-dibromo-2-(2'-thienyl)-3,1-benzoxazin-4(H)-one (2) entirely at position-4, producing the corresponding benzamide derivatives 3a-i. Compound 2 reacted with hydrazoic acid affording the tetrazole 5, beside the benzimidazole derivative 6. Similarly carbon nucleophiles, such as ethyl acetoacetate attack 2 to give 7. 6,8-Dibromo-2(2'-thienyl)-4(3H)-quinazoline and its 3-substituted derivatives 8 a-g were also synthesized. Theoretical calculations for the benzoxazinone 2 and others, based on the simple HMO-method were performed. Close accordance between the theoretically predicted reactivities and the experimental findings was obtained. Biological activities of some of the compounds obtained were also tested.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Bacteria / drug effects
  • Chemical Phenomena
  • Chemistry
  • Microbial Sensitivity Tests
  • Oxazines / chemical synthesis*
  • Oxazines / pharmacology
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology
  • Thiophenes / chemical synthesis*
  • Thiophenes / pharmacology

Substances

  • Anti-Bacterial Agents
  • Oxazines
  • Quinazolines
  • Thiophenes