Bicyclic Pyridines Containing Ring‐Junction Nitrogen

doi:10.1002/9781118686263.ch13

Privileged Structures in Drug Discovery 2018

DOI: 10.1002/9781118686263.ch13

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Bicyclic Pyridines Containing Ring‐Junction Nitrogen

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2022

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Cited by 2 publications

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Regioselective Synthesis of Pyrazolo[1,5-a]pyridine via TEMPO-Mediated [3 + 2] Annulation–Aromatization ofN-Aminopyridines and α,β-Unsaturated Compounds

et al. 2022

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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.

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Regioselective Synthesis of Pyrazolo[1,5-a]pyridine via TEMPO-Mediated [3 + 2] Annulation–Aromatization ofN-Aminopyridines and α,β-Unsaturated Compounds

et al. 2022

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Base-mediated [3 + 2]-cycloannulation strategy for the synthesis of pyrazolo[1,5-a]pyridine derivatives using (E)-β-iodovinyl sulfones

2022

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Bicyclic Pyridines Containing Ring‐Junction Nitrogen

Cited by 2 publications

References 464 publications

Regioselective Synthesis of Pyrazolo[1,5-a]pyridine via TEMPO-Mediated [3 + 2] Annulation–Aromatization ofN-Aminopyridines and α,β-Unsaturated Compounds

Regioselective Synthesis of Pyrazolo[1,5-a]pyridine via TEMPO-Mediated [3 + 2] Annulation–Aromatization ofN-Aminopyridines and α,β-Unsaturated Compounds

Base-mediated [3 + 2]-cycloannulation strategy for the synthesis of pyrazolo[1,5-a]pyridine derivatives using (E)-β-iodovinyl sulfones

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