An Improved H-Phosphonate Approach for Practical Synthesis of Phosphoramidon

被引:0
作者
Sun, Qi [1 ,2 ]
Yang, Qingkun [1 ]
Gong, Shanshan [1 ]
Sun, Jian [1 ]
Li, Xingjian [1 ]
Liu, Guodong [2 ]
机构
[1] Jiangxi Sci & Technol Normal Univ, Jiangxi Key Lab Organ Chem, Nanchang 330013, Jiangxi, Peoples R China
[2] Jiangxi Prov Coll & Univ, High Level Engn Res Ctr Biopharmaceut Mol & Diagn, Nanchang 330013, Jiangxi, Peoples R China
基金
中国国家自然科学基金;
关键词
oxidative coupling; phosphoramidate; inhibitor constant; Phosphoramidon; H-phosphonate; TRANSITION-STATE; THERMOLYSIN; INHIBITOR; BINDING; ANALOGS; STRATEGY;
D O I
10.1080/10426507.2014.902829
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
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.
引用
收藏
页码:1887 / 1894
页数:8
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