Abstract
To discover new natural-product-based pesticides, we structurally modified andrographolide, a labdane diterpenoid isolated from Andrographis paniculata, and stereoselectively prepared a series of 12α-(substituted)benzylamino-14-deoxyandrographolide derivatives (I–V). Three-dimensional structures of compounds 3c, 3d, IIIa and IIIb were further determined by single-crystal X-ray diffraction. Compounds IIa (R1 = n-C3H7, R2 = PhCH2) exhibited more promising insecticidal activity against Mythimna separata than toosendanin. Compounds 3a (R1 = H), Ib (R1 = H, R2 = 4-ClPhCH2), and IVa (R1 = 4-ClPh, R2 = PhCH2) showed potent acaricidal activity against Tetranychus cinnabarinus.
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