title: Synthesis of benzodioxinopyrroles as selective alpha 2-adrenoceptor antagonists.
abstract: A novel series of tetrahydrobenzodioxinopyrroles has been identified as potent and selective alpha 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).
authors.affiliation: Department of Medicinal Chemistry, Glaxo-Wellcome, Stevenage, Hertfordshire, UK.
authors.forename: J
authors.initials: J
authors.lastname: Kitchin
authors.forename: A D
authors.initials: AD
authors.lastname: Borthwick
authors.forename: A C
authors.initials: AC
authors.lastname: Brodie
authors.forename: P C
authors.initials: PC
authors.lastname: Cherry
authors.forename: A J
authors.initials: AJ
authors.lastname: Crame
authors.forename: A J
authors.initials: AJ
authors.lastname: Pipe
authors.forename: P A
authors.initials: PA
authors.lastname: Procopiou
authors.forename: M A
authors.initials: MA
authors.lastname: Seaman
authors.forename: J P
authors.initials: JP
authors.lastname: Turnbull
mesh_terms: D058669:Adrenergic alpha-2 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010883:Piperoxan / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism
chemical_list: D058669:Adrenergic alpha-2 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D011758:Pyrroles; D010883:Piperoxan; C065161:fluparoxan