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. Author manuscript; available in PMC: 2022 Jan 28.
Published in final edited form as: J Med Chem. 2021 Jan 14;64(2):1139–1169. doi: 10.1021/acs.jmedchem.0c01777

Scheme 1:

Scheme 1:

Preparation of building block aminopyrazoles 4.

Conditions: (a) MeCN, n-BuLi, THF, −78 °C to rt; (b) R1NH-NH2, MeOH, 120 °C, microwave or R1NH-NH2·HCl, NEt3, MeOH, 120 °C, microwave.