Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity

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专利权人:

Academia Sinica

发明人:

Cheng, Yih-Shyun Edmond,Fang, Jim-Min,Jan, Jia-Tsrong,Wong, Chi-Huey,Shie, Jiun-Jie

申请号：

AU2008292859

公开号：

AU2008292859B2

申请日:

2008.08.29

申请国别(地区):

AU

年份:

2013

代理人:

摘要：

Novel phosphonate compounds are described. The compounds have activity as neuraminidaseinhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The presentdisclosure also provides an enantioselective synthetic route to known neuraminidaseinhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novelphosphonate compounds, via D-xylose. Another efficient and flexible synthesisof Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was alsoachieved in 11 steps and >； 20% overall yields from the readily available fermentationproduct (1

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