| 文雯,李博,杨蕊,安琪琪,胡家栋.化学通报,2023,86(12):1475-1480,1466. |
| 靶向RET抑制剂塞尔帕替尼的合成进展 |
| Progress in the Synthesis of Targeted RET Inhibitor Selpercatinib |
| 投稿时间：2023-04-24 修订日期：2023-05-17 |
| DOI： |
| 中文关键词: 塞尔帕替尼 RET抑制剂 合成进展 |
| 英文关键词:Selpercatinib, RET inhibitor, Progress in synthesis |
| 基金项目:陕西省重点研发计划项目(2023-YBNY-249)和杨凌职业技术学院院内基金项目(ZK20-72和ZK21-83)资助 |
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| 中文摘要: |
| 塞尔帕替尼是一种高选择性转染过程中重排(RET)受体酪氨酸激酶抑制剂,由Loxo Oncology公司研发于2020年5月在美国获批上市用于治疗RET融合阳性非小细胞肺癌、RET融合阳性甲状腺癌和RET突变甲状腺髓样癌。本文综述了目前报道的有关塞尔帕替尼的合成方法研究进展,并讨论了各方法的特点,以期对其工业化生产提供参考。 |
| 英文摘要: |
| Selpercatinib is a receptor tyrosine kinase RET (rearranged during transfection) inhibitor being developed by Loxo Oncology. Selpercatinib was approved by the US FDA at May 2020 for the treatment of RET fusion-positive non-small-cell lung cancer, RET fusion-positive thyroid cancer and RET-mutant medullary thyroid cancer. This paper reviews the synthetic methods of selpercatinib that reported in recent years, and discusses the characteristic of each method in order to provide a reference for industrial production. |
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