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

Haohuan Yuan,Wei Yao, Xiaomin Zhang,Zhao Wei,Jiayue Xi, Yuanyuan Hao,Xian Liu,Ru Jiang,Huifang Nie

The Journal of Organic Chemistry(2024)

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摘要
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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