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