发明名称 Optically active fluorinated vasoconstrictors, methods for making them, and anesthetic formulations comprising them
摘要 (R)-6F-phenylephrine, essentially free of (S)-6F-phenylephrine, and an anesthetic formulation comprising (R)-6F-epinephrin or (R)-6F-phenylephrine and having improved stability compared to formulations containing their non-fluorinated analog, are disclosed. Further disclosed is a method of providing vasoconstriction in a mammal by administering the anesthetic formulation. The anesthetic composition can include an anesthetic, an (R)-chiral compound having the structure: wherein R<1>, R<2>, and R<4 >are independently selected from -H or -F, at least one of R<1>, R<2>, and R<4 >is -F, and R<3 >is selected from -OH, -H or -F, or a pharmaceutically acceptable salt or ester thereof, said vasoconstrictor being essentially free of the (S)-chiral form. Also, a method of chiral addition of cyanide to a ring-fluorinated phenaldehyde, employing an almond hydroxynitrile lyase enzyme, provided in the form of a reversibly soluble polymer conjugate ((R)-Finezyme(TM)-H series biocatalysts) is disclosed. Several such biocatalysts are disclosed.
申请公布号 US2004002549(A1) 申请公布日期 2004.01.01
申请号 US20020190856 申请日期 2002.07.08
申请人 LENOX HAMILTON J.;TERENTIEVA ELENA;GOLOLOBOV MIKHAIL Y. 发明人 LENOX HAMILTON J.;TERENTIEVA ELENA;GOLOLOBOV MIKHAIL Y.
分类号 A61K31/137;A61K31/167;C07C215/60;C07C217/70;C07C233/18;C07C255/37;C12P13/00;(IPC1-7):A61K31/137;C07C215/46 主分类号 A61K31/137
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