A convenient ‘catch, cyclize, and release’ preparation of 3-thio-1,2,4-triazoles mediated by polymer-bound BEMP

A robust ‘catch, cyclize, and release’ preparation of 3-thioalkyl-1,2,4-triazoles mediated by the polymer-bound base P-BEMP is described. This reengineered synthesis combines the chemical efficiency of the classical synthesis (three steps; three diversity points) with the practical benefits of resin-bound reagents (use of excess reagents to drive reactions to completion, no purification of intermediates, automation-friendly). Key advantages/limitations of this scheme, reagent compatibility, and the results of a representative 64-member combinatorial library are described and presented herein.