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Article Dans Une Revue ACS Omega Année : 2017

Expedited route to fully substituted amino-pyrazole building blocks and their further transformations

Résumé

We report here an efficient and easily reproducible two-step approach to heterocycle-substituted amino-pyrazoles from heterocyclic acetonitriles and their unprecedented subsequent transformations to fully substituted pyrazoles. Such transformations include regioselective derivatization from polyamino derivatives, formation of tetracyclic compounds in up to 45% overall yield, and deaminative transformations through diazotization, followed by arylation through Suzuki–Miyaura cross-coupling and C–H activation, providing arylated pyrazoles in up to 71% yield over four steps. This strategy allows the swift introduction of significant molecular complexity to a range of scaffolds.
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Origine : Publication financée par une institution

Dates et versions

hal-01939736 , version 1 (27-01-2024)

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Olena Kuleshova, Olga Khilya, Yulian Volovenko, Sonia Mallet-Ladeira, Viktoriya Dyakonenko, et al.. Expedited route to fully substituted amino-pyrazole building blocks and their further transformations. ACS Omega, 2017, 2 (12), pp.8911-8927. ⟨10.1021/acsomega.7b01419⟩. ⟨hal-01939736⟩
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