4.7 Article

Total Synthesis of Rucaparib

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JOURNAL OF ORGANIC CHEMISTRY
卷 87, 期 7, 页码 4813-4817

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.2c00083

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  1. National Research Foundation of Korea (NRF) - Korean Government [NRF-2021R1A2C1012984, NRF2021R1A5A6002803]

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This study reports a concise total synthesis of rucaparib, an FDA-approved drug for ovarian and prostate cancers. The desired structure was achieved through key reactions, and the final compound was obtained with commercially available starting materials in a simple procedure, resulting in a high overall yield.
A concise total synthesis of rucaparib, an FDA-approved drug for ovarian and prostate cancers, is reported. TheHeck reaction of the commercially available aryl iodide withacrylonitrile provided the desired (E)-2-aminocinnamonitrile deriva-tive. A subsequent imino-Stetter reaction of the aldimine derived from2-aminocinnamonitrile and aldehyde furnished indole-3-acetonitrilebearing the desired substituents at appropriate positions. Theconstruction of thefinal azepinone scaffold via reduction of thenitrile group followed by seven-membered lactamization affordedrucaparib. Notably, the synthesis of rucaparib is achieved usingcommercially available starting materials in only three separationoperations with 54% overall yield.

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