Synthesis and insecticidal efficacy of pyripyropene derivatives. Part II-Invention of afidopyropen.

The synthesis and insecticidal activity of a series of pyripyropene derivatives with cyclopropanecarbonyloxy group(s) at the C-1, C-7 and/or C-11 position(s) were investigated to find novel insecticides. Insecticidal screening of the synthesized PP derivatives revealed that derivative 13, which had cyclopropanecarbonyloxy groups at the C-1 and C-11 positions and a hydroxyl group at the C-7 position, showed the highest insecticidal activity against aphids in laboratory tests. Finally, we selected 13 as a new insecticide candidate for agricultural sucking pests, which is now commercialized under the common name afidopyropen.