A simple protocol for the Buchwald–Hartwig cross-coupling of (hetero)aryl halides with unprotected aminoglutarimide to afford diverse cereblon binding motifs is disclosed. The development of this C–N cross-coupling method was enabled by high-throughput combinatory screening of solvents, bases, temperatures, and ligands. Scope studies revealed generality across various heteroaryl and aryl halides with the reaction proceeding under mild conditions. In comparison, this method demonstrated strategic superiority over previously reported approaches, as evidenced by a significant decrease in step count from known syntheses in the patent literature.

中文翻译：

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通过高通量实验实现加速氨基戊二酰亚胺 C-N 交叉偶联


公开了（异）芳基卤化物与未受保护的氨基戊二酰胺的 Buchwald-Hartwig 交叉偶联以提供多种脑结合基序的简单方案。这种 C-N 交叉偶联方法的开发是通过对溶剂、碱、温度和配体进行高通量组合筛选来实现的。范围研究表明，在温和条件下进行反应时，各种杂芳基和芳基卤化物具有普遍性。相比之下，这种方法显示出优于以前报道的方法的战略优势，专利文献中已知综合的步数显着减少证明了这一点。