Improved synthesis of YG-056SP, a potent oxazolidinone antibacterial candidate against multi-drug resistant bacteria

An improved process for the synthesis of YG-056SP, a potent oxazolidinone candidate against multi-drug resistant bacteria, is developed. Compared with the original synthetic route, this new approach is two steps shorter, and all of the steps involve simple purifications without column chromatography. More importantly, it avoids the use of explosive azide compounds and expensive metal catalysts. The new reaction conditions are mild and safe, which is more suitable for the scalable synthesis of YG-056SP for preclinical studies.