Synthesis and antitumor activities of α-hydroxyamino phosphine oxides by catalyst-free hydrophosphinylation of
Pengfei Zhao1, Peiyuan Li2, Jian Xiao1
1School of Pharmacy, North China University of Science and Technology, Tangshan, 063210, P. R. China. Chunyanliu@ncst.edu.cn.
Abstract:
Inspired by the diverse bioactivities of α-amino phosphine oxides, an efficient strategy for the synthesis of less researched α-(hydroxyamino)diarylphosphine oxides has been developed and their antitumor activities are explored. Under water as a solvent and catalyst-free conditions, the addition of nitrones and diphenylphosphine oxide occurs smoothly to afford α-(hydroxyamino) diarylphosphine oxides in high yields. This reaction features a wide substrate scope, facile starting materials, atom economy, and easy purification. Moreover, the biological evaluation revealed that two synthesized derivatives 5e and 5f could serve as interesting anti-cancer agents for further development.
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