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

IF 3.6 2区化学 Q1 CHEMISTRY, ORGANIC

Journal of Organic Chemistry Pub Date : 2025-03-04 DOI:10.1021/acs.joc.4c0296210.1021/acs.joc.4c02962

Qian Zhang, and , Meng Tang*,

引用次数: 0

Abstract

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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n -甲苯腙合成5-氨基- 1h -吡唑-4-碳腈及其在伊鲁替尼制备中的应用

研究人员开发了一种制备 5-氨基-1H-吡唑-4-甲腈的简便方法。该反应对多种底物具有兼容性，并能高效制备不同的 5-氨基-1H-吡唑-4-甲腈。伊布替尼是在无钯条件下分六步制备的，总产率为 32.7%。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Organic Chemistry 化学-有机化学

CiteScore

6.20

自引率

11.10%

发文量

1467

审稿时长

2 months

期刊介绍： Journal of Organic Chemistry welcomes original contributions of fundamental research in all branches of the theory and practice of organic chemistry. In selecting manuscripts for publication, the editors place emphasis on the quality and novelty of the work, as well as the breadth of interest to the organic chemistry community.