Combinatorial Synthesis of 2-Acyloxycycloh-exylsulfonamides and Evaluation of Their Fungicidal Activity

摘要

@@ In order to discover fungicides having novel structures, we adopted the method of combining the traditional synthesis with fast mixture library synthesis the research on the structure optimization and the structure-activity relationship of the 2Acyloxycyclohexy-lsulfonamides. Acyl chloride (1, R1 ) was reacted with N-substituted phenyl-2hydroxycycloalkylsulfonamides(2, R2) in dichloromethane under the catalysis of TMEDA and molecular sieve to synthesize N-substituted phenyl-2- acyloxycyclohexylsulfonamides (3). The structure optimization of R1 : 13 N-(2-trifluoromethyl-4chlorinephenyl)-2-acyloxycyclohexylsulfonamides were synthesized which structures were confirmed by 1 H NMR, IR and elemental analyses.