Chinese Journal of Applied Chemistry

Chinese Journal of Applied Chemistry ›› 2009, Vol. 26 ›› Issue (10): 1159-1164.

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Solvent-free Ugi Four-component Synthesis and Insecticidal Activities of Novel Fluorine-Containing Philanthotoxins-12 Derivatives

 LIU Nian-Jin, CAO Song, MA Yan-Ming, SHEN Li, QIAN Xu-Hong   

  1. (Shanghai Key Laboratory of Chemical Biology,Center of Fluorine Chemical Technology,School of Pharmacy,East China University of Science and Technology,Shanghai 200237)
  • Received:2008-09-12 Revised:2008-12-18 Published:2009-10-10 Online:2009-10-10

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Abstract:

Eight novel fluorine-containing PhTX-12 derivatives were prepared under one-pot Ugi four-component solvent-free conditions, followed by the simple removal of the protecting groups in the presence of trifluoroacetic acid. Their structures were identified by 1H NMR, 13C NMR and HRMS. Preliminary bioassays indicated that compound 6b showed 44% and 42% mortality rate against Heliothis armigera and Pieris rapae at a concentration of 100 mg/L.

Key words: Philanthotoxin,solventfree synthesis,Ugi 4-CR,insecticidal activity

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