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    • 27. 发明申请
    • METHOD FOR PREPARING CLOPIDOGREL AND ITS DERIVATIVES
    • 制备焦糖及其衍生物的方法
    • US20110087028A1
    • 2011-04-14
    • US12996733
    • 2009-06-09
    • Soon Ook HwangYoung Jin Kim
    • Soon Ook HwangYoung Jin Kim
    • C07D471/04
    • C07D495/04
    • The present invention relates to a method for preparing Clopidogrel and its derivatives. More particularly, the present invention is a method for preparation of (S)-2-Clopidogrel and its derivatives, which are active inhibitors of platelet aggregation, from an optically active (S)-2-chlorophenyl glycine alkyl ester through hydrolysis of racemic 2-chlorophenylglycine alkyl esters using an enzyme. The present invention employs a simple procedure to prepare Clopidogrel and its derivatives. Because no chiral resolving agents are used except for a small amount of enzyme, the cost of preparation can be reduced. In addition, the present invention is suitable for synthesizing highly optical-active Clopidogrel and its derivatives on a large scale by using optically active (S)-2-chlorophenylglycine alkyl ester obtained in high yield as an intermediate, and is also environmentally friendly since no highly toxic reagents are employed.
    • 本发明涉及氯吡格雷及其衍生物的制备方法。 更具体地,本发明是通过外消旋2的水解从光学活性(S)-2-氯苯基甘氨酸烷基酯制备作为血小板聚集的活性抑制剂的(S)-2-氯吡格雷及其衍生物的方法 - 氯苯基甘氨酸烷基酯。 本发明采用简单的方法来制备氯吡格雷及其衍生物。 由于除了少量的酶以外,不使用手性拆分剂,所以可以降低制备成本。 另外,本发明适用于通过使用以高收率获得的光学活性(S)-2-氯苯基甘氨酸烷基酯作为中间体,大规模合成高光活性氯吡格雷及其衍生物,并且也是环保的 使用高毒性试剂。