High-Throughput Photo- and Electrochemical sp(2)-sp(3) Cross-Electrophile Coupling to Access Novel Tedizolid Analogs

利用高通量光电化学sp(2)-sp(3)交叉亲电偶联反应合成新型泰地唑胺类似物

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Abstract

The development of practical synthetic protocols integrating novel technologies may enable rapid and broad exploration of chemical space in medicinal chemistry campaigns. Cross-electrophile coupling (XEC) allows the diversification of an aromatic core with alkyl halides to increase the sp(3) character. Herein, we apply two alternative approaches via either photo- or electro-catalyzed XEC and showcase their complementarity to access novel tedizolid analogs. The parallel photochemical and electrochemical reactors with high light intensity and constant voltage respectively were chosen to yield good conversions, which allowed access to a wide range of derivatives in a much shorter time frame.

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