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In order to discover new antifungal agrochemicals that could have highly active and novel motifs, thirty-six new 2-acylaminocycloalkylsulfonamides ( IV ) were synthesized. Their structures were characterized and confirmed by  1 H NMR,  13 C NMR, IR, MS, elemental analysis and X-ray single crystal diffraction.  In vitro  and  in vivo  activities against various  Botrytis cinerea  strains were evaluated. Bioassay results revealed that most of the title compounds exhibited excellent  in vitro  fungicidal activity, in which compound  IV-26  showed the highest activity against sensitive, low-resistant, moderate-resistant and high-resistant strains of  B. cinerea  compared with the positive fungicide procymidone. Meanwhile  in vivo  fungicidal activity of compound  IV-31  was better than the commercial fungicides procymidone and chesulfamide in greenhouse trial. The structure activity relationship (SAR) was also discussed and the results were of importance to the structural optimization and development of more potent sulfonamides antifungal agents.

Synthesis, Fungicidal Activity, and Structure Activity Relationship of β-Acylaminocycloalkylsulfonamides against Botrytis cinerea