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    • 4. 发明公开
    • METHOD FOR PREPARING RACEMIC OR OPTICALLY ACTIVE GLYCEROPHOSPHORYL CHOLINE
    • VERFAHREN ZUR HERSTELLUNG VON RACEMISCHEM ODER OPTISCH AKTIVEM GLYCEROPHOSPHORYLCHOLIN
    • EP3106465A1
    • 2016-12-21
    • EP15746936.2
    • 2015-02-05
    • Enzytech, Ltd.
    • HWANG, Soon OokYUN, Dae Myoung
    • C07F9/09C07C211/63
    • C07F9/10C07B2200/07C07F9/091C07F9/3808C07F9/65515C07F9/65742
    • The present invention relates to a method of preparing racemic or optically active D or L-α-glycerophosphorylcholine in large amounts by subjecting choline phosphate or a salt thereof, and racemic or optically highly pure (S) or (R)-3-halo-1,2-propanediol to a substitution reaction in a medium at high temperature in the presence of an inorganic base which increases the activity of the reaction. The method for preparing racemic or optically active D or L-α-glycerophosphorylcholine is cost-effective because of the use of starting materials which are inexpensive compared to those in a conventional method. Moreover, the method is simple and convenient because it is performed via a one-pot reaction without a separate purification process. In addition, it enables a large amount of racemic or optically active D or L-α-glycerophosphorylcholine, or a salt thereof, to be quantitatively produced in a medium without side reactions by using the inorganic base which increases the reaction activity.
    • 本发明涉及一种通过使磷酸胆碱或其盐和外消旋或光学上高纯度(S)或(R)-3-卤代 - 吡咯烷酮制备外消旋或光学活性的D或L-±甘油磷酰胆碱的方法, 1,2-丙二醇在无机碱存在下在高温下在介质中进行取代反应,这增加了反应的活性。 制备外消旋或光学活性的D或L-±甘油磷酰胆碱的方法是成本有效的,因为使用与常规方法相比便宜的原料。 此外,该方法简单方便,因为它是通过一锅反应而不进行单独的纯化过程进行的。 此外,通过使用增加反应活性的无机碱,能够在无副反应的培养基中定量生成大量的外消旋或光学活性的D或L-±甘油磷酰胆碱或其盐。