An efficient route to dipyridone acid HIV integrase inhibitors is developed. The key steps include a onepot three-step formation of the core template (containing one point of structural diversity) followed by a regioselective benzylation and in situ deprotection to afford the title compounds. Biotage 微波合成儀 Initiator+ Biotage 微波合成儀 Initiator Biotage 微波合成儀 Initiator+ Robot 8 Biotage 微波合成儀 Initiator+ Robot 60