During the course of our CCR2 research program we discovered a series of novel 3-amino-azetidinyl glycinamides with potent antagonist activity.  As our work progressed, we found, as others working in the field had reported, that we could replace the terminal benzoyl amide bond with a quinazoline.  In the case of our scaffold this not only opened the door to explore a wide variety of related heterocycles but also obviated the need for an aromatic moiety on the opposite terminus of the molecule.  Herein we report the synthesis of not only the novel quinazoline replacements but also the chemistry developed to explore the SAR of the far end of the pharmacophore.

Synthesis of novel monoaryl CCR2 antagonists

244th National Meeting (2012)

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