2092153-80-3Relevant articles and documents
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.
Pyrazolopyridine derivatives for regulating synthesis activity of estrogen receptor
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Paragraph 0120-0125, (2021/09/15)
The invention relates to the technical field of organic chemistry and medicinal chemistry, and in particular, relates to pyrazolopyridine derivatives for regulating the synthesis activity of an estrogen receptor. According to the specific technical scheme, under the alkaline condition, substituted 1-aminopyridine and an alpha,beta-unsaturated compound are stirred together in the presence of an oxidizing agent, and the substituted pyrazol[1,5-a]pyridine compounds are formed. A one-step synthesis strategy is adopted, the alpha,beta-unsaturated compound is used as a raw material, and a series of pyrazol[1,5-a]pyridine compounds are efficiently and highly selectively synthesized in the presence of an organic oxidant.