Synthesis of 5-Amino-1<i>H</i>-pyrazole-4-carbonitriles from <i>N</i>-Tosylhydrazones and 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.
Authors
- Meng Tang (ORCID: https://orcid.org/0000-0003-4398-3900)
- Qian Zhang (ORCID: https://orcid.org/0000-0001-8606-2808)
Institutions
- Lanzhou University (CN)
Publication Details
- Journal
- The Journal of Organic Chemistry
- Published
- 2025-03-05
- DOI
- https://doi.org/10.1021/acs.joc.4c02962
- Citations
- 1
- Primary Topic
- Chronic Lymphocytic Leukemia Research
- Type
- article
- Field-Weighted Citation Impact
- 1.63
Funders
- National Natural Science Foundation of China