Selective ring N-protection of aminopyrazoles

Article abstract of DOI:10.1016/S0040-4039(03)00988-2

Two simple procedures for the selective protection of the ring N of aminopyrazoles as tert-butoxycarbamate (Boc) in high yields are reported; several other protecting groups (Cbz, Bn, SEM) can be introduced using the one-pot procedure (method B). The N-Boc protected aminopyrazoles are acylated at the exocyclic NH₂ group and subsequently deprotected to give the corresponding 3-acylaminopyrazoles in high yields. This procedure is applicable for the rapid parallel synthesis of 3-acylaminopyrazoles.