Synthesis of Tert-butyl-4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1 H-pyrazol-1-yl)piperidine-1-carboxylate

摘要

Tert-butyl-4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate (1) is an important intermediate in many biologically active compounds such as crizotinib. In this work, compound (1) was synthesized through three steps, using tert-butyl-4-hydroxypiperdine-1-carboxylate as starting material. And the structures of tert-butyl-4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxy late was confirmed by MS and ~1HNMR spectrum. The total yield of the three steps was 49.9%.