Highly enantioselective Rh-catalyzed asymmetric reductive dearomatization of multi-nitrogen polycyclic
Chaochao Xie1, Guiying Xiao1, Qianling Guo1
1Key Laboratory of Radiopharmaceuticals, College of Chemistry, Beijing Normal University No. 19 Xinjiekouwai St. Beijing 100875 China ghhou@bnu.edu.cn dingwanjian@bnu.edu.cn.
Abstract:
A highly enantioselective rhodium-catalyzed reductive dearomatization of 7-substituted pyrazolo[1,5-a]pyrimidines has been realized for the first time by two strategies to afford chiral 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidines with excellent enantioselectivities of up to 98% ee. This method also provides an efficient approach for the synthesis of the powerful BTK inhibitor, zanubrutinib.
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