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- W4212768120 abstract "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." @default.
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- W4212768120 date "2022-02-15" @default.
- W4212768120 modified "2023-10-18" @default.
- W4212768120 title "Regioselective Synthesis of Pyrazolo[1,5-<i>a</i>]pyridine via TEMPO-Mediated [3 + 2] Annulation–Aromatization of <i>N</i>-Aminopyridines and α,β-Unsaturated Compounds" @default.
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- W4212768120 doi "https://doi.org/10.1021/acs.orglett.2c00035" @default.
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