Reaction Conditions for Chemical Coupling (S9155)

Coupling BG-GLA to Amine-containing Precusor

BG-GLA building block contains a reactive carboxy group. Carboxy groups can be activated as acyl halides, acyl azides, acyl imidazoles, anhydrides, esters, etc (1). There are two different ways to couple reactive carboxylic derivatives with an amine-containing precursor. An acyl intermediate can be formed and isolated, then subjected to the reaction with an amine. Alternatively, the acyl intermediate can be generated in situ from the acid by the addition of a activating agent in the presence of an amine. The purification strategy will depend on the label used. Good results have been obtained with both HPLC and silica gel chromatography.