An efficient and convergent route was developed for the synthesis of a novel class of urea-based macrocyclic kinase inhibitors. The synthesis is featured with an efficient urea formation by using a key carbamate intermediate and with a smooth ring-closure olefin metathesis. Furthermore, the hydrogenations of the resulting olefins were investigated in this complex macrocyclic ring system.
开发了一条高效且收敛的合成路线,用于制备一类新型基于
尿素的巨环激酶
抑制剂。该合成方法的特色是通过使用关键的
氨基甲酸酯中间体实现高效的
尿素形成,并通过顺畅的环合烯烃复分解反应。此外,还研究了在这种复杂的巨环体系中所得烯烃的氢化反应。