A short scalable biomimetic route to bioactive natural product bimagnolignan (1) was accomplished. Compound 1 was successfully prepared through a three-step metal-free synthesis from honokiol (2). Alternatively, 1 was also synthesized by biomimetic transformations that mimic tyrosinase in four steps. The key reactions feature a regioselective acetylation, a highly efficient C(sp²)–H oxidation, a cascade aerobic oxidative cyclization/coupling, and a Cu-catalyzed direct oxidative coupling. In addition, cell-based assays validate that 1 is a promising natural lead for HER2-positive breast cancer treatment.

中文翻译：

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双木脂素的仿生全合成：天然抗乳腺癌药物

完成了一种生产生物活性天然产物双木脂素 ( 1 )的短距离可扩展仿生路线。以和厚朴酚为原料，通过三步无金属合成成功制备了化合物1 ( 2 )。或者，1也可以通过仿生转化来合成，该仿生转化分四个步骤模拟酪氨酸酶。关键反应包括区域选择性乙酰化、高效C(sp ² )–H氧化、级联有氧氧化环化/偶联以及Cu催化的直接氧化偶联。此外，基于细胞的检测证实1是治疗 HER2 阳性乳腺癌的一种有前景的天然先导药物。