A Bifunctional Metal/Acid Catalyst for One-pot Multistep Synthesis of Pharmaceuticals

摘要

One inhibitor of the fatty acid transporter FATP4 was synthesized in a three steps one-pot process in the presence of a bifunctional metal/acid catalyst. This molecule which has potential interest for the treatment of the obesity in orlistat (Xenical(TM)) analogue-based therapies has a 3,4-dihydropyrimidin-2(1H)-one (DHPM) scaffold and was obtained by means of a three one-pot process through successive oxidation, cyclocondensation and transesterification reactions. The one-pot strategy was extended to the synthesis of a series of related ester DHPM derivatives.