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Synthesis of MDM2-p53 Inhibitor BI-0282 via a Dipolar Cycloaddition and Late-Stage Davis–Beirut Reaction
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2022-07-07 , DOI: 10.1021/acs.oprd.2c00192
Juergen Ramharter 1 , Michael Kulhanek 1 , Maike Dettling 1 , Gerhard Gmaschitz 1 , Jale Karolyi-Oezguer 1 , Harald Weinstabl 1 , Andreas Gollner 1
Affiliation  

Herein, we report the structure and synthesis of the potent MDM2-p53 inhibitor BI-0282. The complex spirooxindole scaffold bearing four stereocenters embedded in a rigid polycyclic ring-system was effectively prepared on a multi-gram scale in only five synthesis steps employing a three-component 1,3-dipolar cycloaddition and a late-stage Davis–Beirut reaction as key steps.

中文翻译:

通过偶极环加成和晚期戴维斯-贝鲁特反应合成 MDM2-p53 抑制剂 BI-0282

在此,我们报告了有效的 MDM2-p53 抑制剂 BI-0282 的结构和合成。使用三组分 1,3-偶极环加成和后期戴维斯-贝鲁特反应,仅在五个合成步骤中有效地制备了嵌入刚性多环环系统中的带有四个立体中心的复杂螺氧吲哚支架。关键步骤。
更新日期:2022-07-07
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