2092835-01-1Relevant academic research and scientific papers
Regioselective Synthesis of Pyrazolo[1,5- a]pyridine via TEMPO-Mediated [3 + 2] Annulation-Aromatization of N-Aminopyridines and α,β-Unsaturated Compounds
Wang, Amu,Liu, Ya-Zhou,Shen, Zhongke,Qiao, Zeen,Ma, Xiaofeng
supporting information, p. 1454 - 1459 (2022/03/01)
A TEMPO-mediated [3 + 2] annulation-aromatization protocol for the preparation of pyrazolo[1,5-a]pyridines from N-aminopyridines and α,β-unsaturated compounds was developed. The procedure offered multisubstituted pyrazolo[1,5-a]pyridines in good to excellent yield with high and predictable regioselectivity. The modification of marketed drugs including Loratadine, Abiraterone, and Metochalcone, and a one-pot three-step gram scale synthesis of key intermediate for the preparation of Selpercatinib were demonstrated. Mechanism studies show that TEMPO serves both as a Lewis acid and as an oxidant.
INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR KINASES
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, (2021/12/28)
Provided herein are heteroaryl inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
