Facile synthesis of sulfonamide libraries using a solid-polymer-supported HOBt scaffold

Abstract

Using solid-phase synthetic methods, silica-bound 1-hydroxybenzotriazole (Si-HOBt) was prepared by coupling 3-aminopropyl silica gel with 1-hydroxybenzotriazole-6-carboxylic acid (HOBt-COOH). The Si-HOBt was activated by the reaction of Si-HOBT with 3,4-dihydroxy-9,10-dioxo-anthracenesulfonyl chloride (alizarin red S chloride), resulting in the activated Si-HOBt reagent. The reagent was used to prepare a combination library of sulfonamide derivatives of selected aliphatic and aromatic amines for the development of new therapeutics.

Keywords

• Solid-Phase Synthesis
• HOBt
• Sulfonamides Library
• Drug libraries
• HPLC-UV
• Combinatory Chemistry