Stereospecific reduction of Sapogen-3-ones
    8.
    发明申请
    Stereospecific reduction of Sapogen-3-ones 失效
    皂苷-3-酮的立体特异性还原

    公开(公告)号:US20060041119A1

    公开(公告)日:2006-02-23

    申请号:US10531086

    申请日:2003-04-28

    IPC分类号: C07J71/00

    CPC分类号: C07J71/0005

    摘要: A method to stereospecifically prepare a steroidal sapogenin or a derivative thereof by reducing a 3-keto,5β-H steroidal sapogenin with a hindered organoborane or an organo-aluminium hydride. A 3β-hydroxy,5β-H steroidal sapogenin or derivative thereof may be prepared by reducing the 3-keto,5β-H steroidal sapogenin using as reducing agent a relatively highly hindered organoborane reagent or by SN 2 inversion of a 3α-hydroxy,5β-H steroidal sapogenin or derivative thereof. The organo-aluminium hydride may be used to prepare a 3α,5β-H steroidal sapogenin or derivative thereof. The invention provides a convenient route to useful steroidal sapogenins such as sarsasapogenin, episarsasapogenin, smilagenin, epismilagenin and esters thereof, from readily available or easily preparable starting materials (e.g. diosgenone, preparable from diosgenin).

    摘要翻译: 通过用受阻的有机硼烷或有机氢化铝还原3-酮基,5β-H甾体皂苷元,立体选择性地制备甾体皂苷元或其衍生物的方法。 可以通过使用相对高度受阻的有机硼烷试剂的还原剂或通过3α-羟基,5β的SN 2反转来还原3-酮基,5β-H甾体皂苷元来制备3β-羟基,5β-H甾体皂苷元或其衍生物 -H甾体皂苷元或其衍生物。 有机铝氢化物可用于制备3α,5β-H甾体皂苷元或其衍生物。 本发明提供了从易得的或易于制备的起始物质(例如,由薯os皂苷配制的脱水梭子),可用于甾体皂苷元的方便途径,例如萨洒皂草配基,季节调节素,镰刀菌素,epismilagenin及其酯。

    OPHTHALMIC FORMULATIONS
    9.
    发明申请
    OPHTHALMIC FORMULATIONS 审中-公开
    眼科配方

    公开(公告)号:US20140255332A1

    公开(公告)日:2014-09-11

    申请号:US14239288

    申请日:2012-08-24

    IPC分类号: A61K31/79

    摘要: There is provided inter alia a germicidal aqueous formulation, suitable for use in the eye, which has a pH of from 4.0 to 6.5 and which comprises 4.0 to 7.5% w/w of povidone-iodine and a viscosity increasing agent, the formulation buffered with a buffer concentration of 25 mM to 75 mM.

    摘要翻译: 特别提供适用于眼睛的杀菌含水制剂,其具有4.0至6.5的pH,并且其包含4.0至7.5重量%的聚维酮碘和增粘剂,所述制剂用 缓冲液浓度为25mM至75mM。