An Improved H-Phosphonate Approach for Practical Synthesis of Phosphoramidon

作者:Sun, Qi*; Yang, Qingkun; Gong, Shanshan; Sun, Jian; Li, Xingjian; Liu, Guodong
来源:Phosphorus, Sulfur, and Silicon and the Related Elements, 2014, 189(12): 1887-1894.
DOI:10.1080/10426507.2014.902829

摘要

An improved synthetic method based on glycosyl-1-H-phosphonate monoester intermediate has been developed for the multigram-scale preparation of phosphoramidon, a naturally occurring phosphorus-linked glycodipeptide. The inhibitor constant of the synthetic sample against thermolysin established that a high level of biological activity can be obtained following this synthetic method.

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