The Iliopoulos laboratory previously reported the discovery of compound 76, a small molecule HIF2α inhibitor. HIF2α activation is known to play a critical role in both von Hippel-Lindau (VHL) disease-related tumors and sporadic renal cell carcinoma (RCC). We required a facile and scalable synthetic route to confirm the structure, to investigate the biological properties of compound 76, and to perform structure activity relationship optimization studies. Herein, we report the straightforward synthesis of compound 76 and a preliminary investigation into the scope of the methods developed.

中文翻译：

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通过Japp-Klingemann偶联合成HIF-2α翻译抑制剂化合物76

Iliopoulos实验室先前曾报告发现了化合物76，这是一种小分子HIF2α抑制剂。已知HIF2α激活在von Hippel-Lindau（VHL）疾病相关的肿瘤和散发性肾细胞癌（RCC）中均起关键作用。我们需要一种简便且可扩展的合成路线来确认结构，研究化合物76的生物学特性并进行结构活性关系优化研究。本文中，我们报告了化合物76的直接合成方法，并对所开发方法的范围进行了初步研究。