Abstract The synthesis of [1-15 N, 2-13 C]-difloxacin, an arylfluoroquinolone antibacterial agent, is reported. As a crucial initial step, the starting materials ethyl 2, 4, 5- trifluorobenzoylacetate,[formyl-13 C]-triethyl orthoformate, and [15 N]-4-fluoroaniline were reacted to ethyl [15 N, 3-13 C]-3-(4-fluoroanilino)-2-(2, 4, 5-trifluorobenzoyl) acrylate. After cyclization and ester cleavage, the resulting intermediate was reacted with 1- ...
[Renau, Thomas E.; Sanchez, Joseph P.; Shapiro, Martin A.; Dever, Julie A.; Gracheck, Stephen J.; Domagala, John M. Journal of Medicinal Chemistry, 1995 , vol. 38, # 15 p. 2974 - 2977]
[Renau, Thomas E.; Sanchez, Joseph P.; Shapiro, Martin A.; Dever, Julie A.; Gracheck, Stephen J.; Domagala, John M. Journal of Medicinal Chemistry, 1995 , vol. 38, # 15 p. 2974 - 2977]