Preparation process of HER2 small-molecule inhibitor Fikatinib

The invention provides a preparation process of an HER2 small-molecule inhibitor graphic-batatinib. Compared with the prior art, in the step (1), the compound shown in the formula 1, the compound shown in the formula 2, triphenylphosphine and diethyl azodicarboxylate are contacted, a Mitsunobu reaction is adopted, phenolic hydroxyl groups can be specifically reacted, the reaction site is single, the defect that heating is needed in the halogenation reaction can be avoided, and the method has the advantages of being mild in condition, high in yield and the like. And the operation is simple. The synthetic route and the preparation process have the advantages of short steps, mild conditions and easiness in operation, and can be suitable for the operability of industrial mass production. 本发明提出一种HER2小分子抑制剂图卡替尼的制备工艺。相对于现有技术，本发明的发明人在步骤(1)中，将式1所示化合物、式2所示化合物、三苯基膦、偶氮二甲酸二乙酯进行接触，采用Mitsunobu反应，其可特异性的将酚羟基进行反应，反应位点单一，不仅可以避免卤化反应需要加热的缺点，还具有条件温和，操作简单的优势。本发明所述的合成路线和制备工艺，具有步骤短，条件温和，易操作的优势，可适用于工业化大生产的操作性。