Synthesis of 1-aroyl(1-arylsulfonyl)-4-bis(trifluoromethyl)alkyl semicarbazides as potential physiologically active compounds

1,1-Bis(trifluoromethyl)alkyl isocyanates obtained from perfluoroisobutene (PFIB) react with aroyl(arylsulfonyl)hydrazines. Twenty eight prospective biologically active polyfluorinated 1,4-substituted semicarbazides were synthesized. The structure of each new product was confirmed by analytical and spectroscopic methods. The Lipinski's and Gelovani's parameters were then calculated. Two adjustments to the Lipinski rules of five are suggested for fluorinated drug candidates. (C) 2013 Elsevier B.V. All rights reserved.