The utilization of ball milling in synthesis of aryl guanidines through guanidinylation and N-Boc-deprotection sequence

摘要

Solid state ball milling was used in guanidinylation reactions of aromatic amines with N,N'-Di-Boc-1H-pyrazole-1-carboxamidine reagent. Reaction conditions are advantageous, and in general reactions proceed in significantly shorter reaction times and in higher yields than under the conventional solution conditions. Mechanochemical conditions were also successfully applied to the cleavage of N-Boc protecting group. (C) 2018 Elsevier Ltd. All rights reserved.