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.
Seelen, Werner,Sch?fer, Martina,Ernst, Alexander
p. 4491 - 4493
(2007/10/03)
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