Synthesis of Substituted Pyrimido[1,2‐b]indazoles through (3+2+1) Cyclization of 3‐Aminoindazoles, Ketones, and N,N‐Dimethylaminoethanol as One‐Carbon Synthon

2‐Mono‐ or 2,3‐disubstituted pyrimido[1,2‐b]indazoles are synthesized by a (3+2+1) three‐component cyclization of 3‐aminoindazoles, ketones, and N,N‐dimethylaminoethanol as a methine source. The reaction demonstrates good tolerance of both aromatic and aliphatic ketones, as well as various substitut...

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Veröffentlicht in:Advanced synthesis & catalysis 2022-09, Vol.364 (18), p.3263-3272
Hauptverfasser: Qin, Zemin, Ma, Renchao, Ying, Shenpeng, Li, Fanzhu, Ma, Yongmin
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Sprache:eng
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Zusammenfassung:2‐Mono‐ or 2,3‐disubstituted pyrimido[1,2‐b]indazoles are synthesized by a (3+2+1) three‐component cyclization of 3‐aminoindazoles, ketones, and N,N‐dimethylaminoethanol as a methine source. The reaction demonstrates good tolerance of both aromatic and aliphatic ketones, as well as various substitution patterns in air. A plausible mechanism is discussed.
ISSN:1615-4150
1615-4169
DOI:10.1002/adsc.202200707