Synthesis of 5‑Amino‑1<i>H</i>‑pyrazole-4-carbonitriles from <i>N</i>‑Tosylhydrazonesand Its Application in the Preparation of Ibrutinib

A facile method for preparing 5-amino-1<i>H</i>-pyrazole-4-carbonitriles was developed. The reaction exhibited compatibility to various substrates, and different 5-amino-1<i>H</i>-pyrazole-4-carbonitriles were prepared efficiently. Ibrutinib was prepared under palladium-free conditions in six steps in 32.7% overall yield.

Publication Details

Journal
Figshare
Published
2025-03-05
DOI
https://doi.org/10.1021/acs.joc.4c02962.s001
Primary Topic
Multicomponent Synthesis of Heterocycles
Type
article
Field-Weighted Citation Impact
0.00
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article

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

Figshare
Multicomponent Synthesis of Heterocycles
article

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

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Abstract

A facile method for preparing 5-amino-1<i>H</i>-pyrazole-4-carbonitriles was developed. The reaction exhibited compatibility to various substrates, and different 5-amino-1<i>H</i>-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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Openalex Percentile: Top 60%
Multicomponent Synthesis of Heterocycles
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Synthesis of 5‑Amino‑1<i>H</i>‑pyrazole-4-carbonitriles from <i>N</i>‑Tosylhydrazonesand Its Application in the Preparation of Ibrutinib · Figshare (2025) | TGRS Research Map | TGRS