Chinese Journal of Applied Chemistry ›› 2020, Vol. 37 ›› Issue (8): 877-882.DOI: 10.11944/j.issn.1000-0518.2020.08.200056

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One-Pot Synthesis of Aryl/Heteroaryl Aminomethylene Bisphosphonates

ZHANG Baohua, SHI Lanxiang*   

  1. College of Chemical Engineering,Shijiazhuang University,Shijiazhaung,Hebei 050035,China
  • Received:2020-02-28 Published:2020-08-01 Online:2020-08-07
  • Contact: SHI Lanxiang, professor; Tel:0311-66617323;; Research interests:drug synthesis
  • Supported by:
    Hebei Province Science and Technology Support Project(No.18271404D)

Abstract: A number of aryl/heteroaryl aminomethylene bisphosphonates were synthesized by one-pot reaction of diverse aryl/heteroaryl amines with diethyl phosphite and triethyl orthoformate in the presence of I2 under solvent free conditions. The product yields are 96%~99%. When the molar fraction of I2 is 5%, the product yield is the highest. The procedure is simple and the substrate scope is large. I2 is safe and very efficient as the catalyst.

Key words: aryl/heteroaryl aminomethylene bisphosphonates, I2, one-pot synthesis, solvent free