Preparation method of targeted drug BLU-667

The invention discloses a preparation method of a targeted drug BLU-667. The preparation method comprises the following steps: firstly, carrying out BOC protection on amino of 2-chloro-4-methyl-6-aminopyrimidine, carrying out carbon-carbon coupling on the obtained intermediate 1 and an iodo compound under the catalysis of organic zinc and palladium catalysts to obtain an intermediate 2, then carrying out BOC protection removal, diazotization reaction and hydrolysis to convert the amino into hydroxyl to obtain an intermediate 3, carrying out Mitsunobu reaction and BOC removal to obtain an intermediate 4, and finally, carrying out amide condensation to obtain the BLU-667. According to the invention, the synthesis steps are reduced, the use of harmful compounds is reduced, the production cost is reduced, the production operation is optimized, and the yield is improved. 本发明公开了一种靶向药物BLU-667的制备方法。本发明首先将2-氯-4-甲基-6-氨基嘧啶的氨基进行BOC保护，得到的中间体1与碘代物在有机锌和钯催化剂催化下碳碳偶联得到中间体2，然后脱BOC保护、重氮化反应及水解将氨基转化为羟基得到中间体3，再经光延反应及脱BOC得到中间体4，最后经酰