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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

ADVANCED SYNTHESIS & CATALYSIS(2022)

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摘要
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.
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关键词
annulation, multi-component reaction, pyrimido[1, 2-b]indazole, (3+2+1) cyclization, carbon synthon, N, N-dimethylaminoethanol
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