SAR studies on thiazolo[4,5-d]pyrimidine based CXCR2 antagonists involving a novel tandem displacement reaction

As part of a Lead Optimisation programme to identify small molecule antagonists of the human CXCR2 receptor, a series of substituted thiazolo[4,5-d]pyrimidines was prepared via the application of a novel tandem displacement reaction.

Graphical abstractThe optimisation of antagonists of the CXCR2 receptor is described involving a novel tandem displacement reaction culminating in the synthesis of 6, a novel, potent and metabolically stable lead compound.Figure optionsDownload full-size imageDownload as PowerPoint slide