An efficient method for preparing the sphingosine-1-phosphate receptor agonist, KRP203-phosphate

An efficient method for mono-phosphorylation of 2 (KRP203) using cbz-protection, dibenzylphosphoryl chloride and TMSI affording 2-P (KRP203-P) was developed. We applied the present method to the synthesis of KRP203 phosphate analogs which were difficult to produce through tradition procedures.

A three-step procedure for the preparation of mono-phosphorylation of KRP203 to 2-P has been developed. This method was considered as an effective route to synthesize various analogs of 2-P.Figure optionsDownload as PowerPoint slide