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    SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY
    4.
    发明专利
    SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY 未知

    公开(公告)号：CA2697837C

    公开(公告)日：2016-08-16

    申请号：CA2697837

    申请日：2008-08-29

    Applicant: ACADEMIA SINICA

    Inventor： WONG CHI-HUEY ,  FANG JIM-MIN ,  SHIE JIUN-JIE ,  CHENG YIH-SHYUN EDMOND ,  JAN JIA-TSRONG

    IPC: A61K31/662 ,  A61P31/16

    Abstract: Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and > 20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5-cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio-- and stereoselective bromoamidation of a bromoarene cis- dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.

    SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY
    10.
    发明专利
    SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY 未知

    公开(公告)号：CA2697837A1

    公开(公告)日：2009-03-05

    申请号：CA2697837

    申请日：2008-08-29

    Applicant: ACADEMIA SINICA

    Inventor： WONG CHI-HUEY ,  FANG JIM-MIN ,  SHIE JIUN-JIE ,  CHENG YIH-SHYUN EDMOND ,  JAN JIA-TSRONG

    IPC: A61K31/7076 ,  A61K9/16 ,  A61K31/70 ,  A61K31/7052 ,  C07C233/52 ,  C07C247/14 ,  C07H19/04

    Abstract: Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and > 20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5- cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis- dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.

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