One-Pot Synthesis of Aryl/Heteroaryl Aminomethylene Bisphosphonates

doi:10.11944/j.issn.1000-0518.2020.08.200056

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^*

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; E-mail:kedashilanxiang@163.com; Research interests:drug synthesis
Supported by:
Hebei Province Science and Technology Support Project(No.18271404D)

Abstract

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

ZHANG Baohua, SHI Lanxiang. One-Pot Synthesis of Aryl/Heteroaryl Aminomethylene Bisphosphonates[J]. Chinese Journal of Applied Chemistry, 2020, 37(8): 877-882.

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One-Pot Synthesis of Aryl/Heteroaryl Aminomethylene Bisphosphonates

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