N,N-DI(2-CHLOROETHYL)-N-MORPHOLYL-N-CYCLOHEXYLTRIAMIDES OF PHOSPHORIC ACID SHOWING ANTIINFLAMMATORY ACTIVITY Russian patent published in 1994 - IPC

FIELD: organophosphorus compounds. SUBSTANCE: synthesis is carried out from dichloroanhydride of N, N-di(2-chloroethyl)amidophosphoric acid and aminocyclohexane or ethyl ester of cis-4-amino-cyclohexane carboxylic acid in the medium of absolute ether at -5-0 C following by treatment with morpholine. The yield, % ; m. p. , C; gross-formula: 1 a) 65; 132-136 (in benzene); C₁₄H₂₈Cl₂N₃O₂P; 1b) 54; 94 (in ether); C₁₇H₃₂Cl₂N₃O₄P. New compounds show antiinflammatory activity: for 1a effective dose ED₅₀ = 8 mg/kg at toxicity LD₅₀ = 650 mg/kg (intraperitoneally). Therapeutic index for 1a and 1b is 81 and 58, respectively, that shows great spectrum of pharmacological action. EFFECT: synthesis of compounds of class indicated above showing enhanced activity and lowered toxicity. 2 tbl