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Published on: October 31, 2014
A highly efficient nucleophilic substitution reaction between R2P(O)H and triarylmethanols to synthesize
Long Chen1, Xin-Yue Fang, Yun-Xiang Zou
1Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics Chengdu University, 168 Hua Guan Road, Chengdu 610052, P. R. China. chenlong@cdu.edu.cn.
Abstract:
A highly efficient and general nucleophilic substitution reaction between dialkyl H-phosphonates or diarylphosphine oxides and triarylmethanols catalyzed by HOTf (trifluoromethanesulfonic acid) has been developed. It provides an atom-economical protocol for the synthesis of various symmetrical and unsymmetrical phosphorus-substituted triarylmethanes that constitute an emerging family of potent anticancer agents in rich diversity with 40 to 96% yields. The synthetic applicability of this protocol is demonstrated by gram-scale preparations.
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