We report the scalable, high-yielding, and highly selective synthesis of the β-lactamase inhibitor QPX7728 featuring two key synthetic steps: nickel-catalyzed boron insertion of benzofuran 1 followed by enantioselective cyclopropanation of the resulting cyclic vinylboronate 2. The identification of the key reagents (catalyst and chiral auxiliary) for both steps relied on the use of high-throughput experimentation. Further optimization allowed for the cost-effective and scalable production of QPX7728.

中文翻译：

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通过连续镍催化硼插入苯并呋喃底物和所得乙烯基硼酸酯的对映选择性环丙烷化合成 β-内酰胺酶抑制剂 QPX7728

我们报告了 β-内酰胺酶抑制剂 QPX7728 的可扩展、高产和高选择性合成，其具有两个关键合成步骤：镍催化硼插入苯并呋喃1，然后对所得环状乙烯基硼酸酯2进行对映选择性环丙烷化。两个步骤的关键试剂（催化剂和手性助剂）的识别依赖于高通量实验的使用。进一步优化使 QPX7728 的生产具有成本效益和可扩展性。