Development of various five- and six-membered lactams, containing quaternary centers, was required in order to drive SAR for desirable PK/PD properties for the EP3 antagonist program for Type II diabetes.  The synthesis team enabled several viable strategies which led to the discovery of PF-6748962 and PF-06747524, both containing a six-membered lactam bearing a chiral quaternary carbon in the alpha position.  The enabled syntheses were also scaled up to &gt;200g to supply key in vivo studies for the program.  The various strategies explored to synthesize the lactams will be discussed. <br/>

Synthetic enablement of lactam templates to drive SAR for an EP3 antagonist program

256th National Meeting (2018)

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