Over the past two decades 2-amino-3-benzoylthiophenes have been found to act as allosteric enhancers of the adenosine A₁ receptor (A₁AR). As such, compounds of this type have potential applications in the therapy of a variety of disorders by enhancing A₁AR activation. Initial studies in this field identified various 2-amino-3-benzoylthiophenes as potential leads and of these PD 81723 1a has become the benchmark for comparative studies due to its favourable ratio of allosteric enhancement to antagonism. Surprisingly the synthesis and characterization of PD 81723 1a has not been previously reported. Herein we report the synthesis and characterization of this important A₁AR allosteric enhancer. As part of this study we also found an unexpected reaction pathway to 2-phenylthiophene-3-carbonitriles.