Late-stage derivatization of pharmaceutically relevant scaffolds relies on the availability of highly functional-group tolerant reactions. Reactions that increase the sp3 character of molecules enable the pursuit of more selective and well-tolerated pharmaceuticals. Herein, we report the use of sp3-sp2 cross-electrophile reductive couplings to modify a generic ATP-competitive kinase inhibitor with a broad range of primary and secondary alkyl halide coupling partners.

中文翻译：

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还原性sp3-sp2偶联反应可实现药物的后期修饰。

药物相关支架的后期衍生化依赖于高度官能团耐受的反应的可用性。增加分子sp3特性的反应使人们能够追求更具选择性和耐受性的药物。在这里，我们报告使用sp3-sp2亲电还原还原偶联来修饰具有广泛范围的一级和二级烷基卤化物偶联伙伴的通用ATP竞争性激酶抑制剂。