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Highly Enantioselective Ir-Catalyzed Hydrogenation of Pyrazolo[1,5‑a]pyrimidine for the Synthesis of Zanubrutinib

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posted on 2024-01-24, 02:03 authored by Haohuan Yuan, Wei Yao, Xiaomin Zhang, Zhao Wei, Jiayue Xi, Yuanyuan Hao, Xian Liu, Ru Jiang, Huifang Nie
A highly enantioselective catalytic reduction of pyrazolo[1,5-a]pyrimidine to zanubrutinib has been realized by the Ir/(R)-t-Bu-FcPhox complex. This chiral product could be obtained in up to >99% ee in the asymmetric transformation without any other additives, providing a new route for the asymmetric synthesis of zanubrutinib.

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