Synthesis of 5-Amino-1H-pyrazole-4-carbonitriles from N-Tosylhydrazones and Its Application in the Preparation of Ibrutinib

被引:0
|
作者
Zhang, Qian [1 ]
Tang, Meng [1 ]
机构
[1] Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China
基金
中国国家自然科学基金;
关键词
ALKYLATED TOSYLHYDRAZONES; VERSATILE REAGENTS; PYRAZOLES;
D O I
10.1021/acs.joc.4c02962
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A facile method for preparing 5-amino-1H-pyrazole-4-carbonitriles was developed. The reaction exhibited compatibility to various substrates, and different 5-amino-1H-pyrazole-4-carbonitriles were prepared efficiently. Ibrutinib was prepared under palladium-free conditions in six steps in 32.7% overall yield.
引用
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页数:4
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