Synthesis of Benzodioxinopyrroles as selective α2-adrenoceptor antagonists

A novel series of tetrahydrobenzodioxinopyrroles has been identified as potent and selective α 2 -adrenoceptor antagonists. Convergent syntheses have been developed that allowed the preparation of analogues and their enantiomers. A compound of particular interest is the 5-fluoro substituted analogue (fluparoxan).