A Convenient Method for the Synthesis of Aminomethylmonoalkylphosphinate

Authors

  • Derong Ding,

    1. Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Rose Street, Lexington, KY 40536-0082, USA
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  • Guang Yan

    Corresponding author
    1. Department of Biomedical and Pharmaceutical Sciences, Idaho State University; Pocatello, Idaho 83209, USA
    • Department of Biomedical and Pharmaceutical Sciences, Idaho State University; Pocatello, Idaho 83209, USA, Tel: +1-208-282-2681
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Abstract

Starting from the readily available 4-methylbenzoic acid, an efficient protocol for the preparation of ethyl 4-(aminomethyl) benzyl (methyl) phosphinate (1), a novel aminomethylmonoalkylphosphinate was reported in this communication. The important step involves the selective monochlorination of phosphonic ester by POCl3 and forming the phosphonochloridate, and followed by nucleophilic addition of CH3MgBr to the acid chloride intermediate.

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