抗肿瘤新药Larotrectinib合成方法简评

A review of Larotrectinib Synthesis Methods for Antitumor Drugs

Larotrectinib是一种广谱的抗肿瘤药,其在TRK融合肿瘤中具有一致和持久的抗肿瘤活性,适用的患者年龄和肿瘤类型范围广,并且具有良好的耐受性,有望成为第一个通过"篮子"临床试验(basket trial)获批的靶向药物。本文介绍了目前已报道的Larotrectinib合成路线,并对其进行分析讨论,以期望找到最合适的工业化生产路线。

Larotrectinib is a broad-spectrum antitumor drug, has a consistent and lasting antitumor activity in TRK fusion in the tumor, patient age and tumor type scope is wide, and has a good tolerance, is expected to become the first through the ＂basket＂ （basket trial） clinical trials of targeted drugs approved. In this paper, the synthetic route of Larotrectinib has been reported and analyzed and discussed, with a view to finding the most suitable route for industrial production.