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
来源：
JOURNAL OF ORGANIC CHEMISTRY | 2025年
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.
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页数：4
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