Novel synthesis of 3,4-dihydro-5-bromo[1,4]oxazin-2-one derivatives, new protease inhibitor scaffold

Abstract

We designed and synthesized a new class of serine protease inhibitors based on the oxazinone core. To this end, we first developed a short and efficient route to synthesize a new 3,4-dihydro[1,4]oxazin-2-one ring. Then we successfully synthesised the corresponding 5-bromo derivatives which have never been reported before, and demonstrated their inhibitory activities on α-chymotrypsin.