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    • 2. 发明授权
    • Method for the synthesis of phospholipid ethers
    • 磷脂醚合成方法
    • US07893286B2
    • 2011-02-22
    • US12156287
    • 2008-05-30
    • Anatoly PinchukJamey P. WeichertMarc Longino
    • Anatoly PinchukJamey P. WeichertMarc Longino
    • C07F9/02
    • C07F9/10
    • Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.
    • 公开了用于合成磷脂醚类似物和烷基磷酸胆碱类似物的改进方法。 所述方法允许所用反应物具有更大的通用性,并且更容易合成不同长度的烷基链,同时在室温或更低温度下提供反应温度。 本文公开的方法提供使用烷基卤和有机锌试剂的反应物和条件,因此不利用Gringard反应,从而更容易地分离和纯化产物。 通过本文公开的方法合成的PLE化合物也可用于合成高比活性磷脂醚(PLE)类似物,用于治疗和诊断癌症。