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METHOD FOR PREPARING ANTI-ANGIOGENIC COMPOUND AND INTERMEDIATE THEREOF
METHOD FOR PREPARING ANTI-ANGIOGENIC COMPOUND AND INTERMEDIATE THEREOF
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机译:一种抗血管生成化合物及其中间体的制备方法
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摘要
Disclosed is a method for preparing an anti-angiogenic compound represented by formula (I). The method comprises the step of reacting a compound of formula (II) with a compound of formula (III) in the presence of Cs2CO3 in a polar organic solvent to produce the compound of formula (I). According to the method of the present invention, by reacting the compound of formula (III) with the compound of formula (II) directly without protecting amino group in the compound of formula (III) under a certain condition, the yield is greatly improved, the synthetic method becomes simpler, the cost is also greatly reduced, and the commercial synthesis of the compound of formula (I) becomes possible. The preparation method for intermediate thereof is also disclosed.
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机译:公开了一种制备由式(I)表示的抗血管生成化合物的方法。该方法包括以下步骤:在极性有机溶剂中,在Cs 2 CO 3存在下,使式(II)的化合物与式(III)的化合物反应,以制备式(I)的化合物。根据本发明的方法,通过在一定条件下使式(III)的化合物与式(II)的化合物直接反应而不保护式(III)的化合物中的氨基,大大提高了产率,合成方法变得更简单,成本也大大降低,式(I)化合物的商业合成成为可能。还公开了其中间体的制备方法。
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