Synthesis of benzodioxinopyrroles as selective alpha 2-adrenoceptor antagonists.
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).
Kitchin
J
J
Department of Medicinal Chemistry, Glaxo-Wellcome, Stevenage, Hertfordshire, UK.
Borthwick
A D
AD
Brodie
A C
AC
Cherry
P C
PC
Crame
A J
AJ
Pipe
A J
AJ
Procopiou
P A
PA
Seaman
M A
MA
Turnbull
J P
JP
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
D058669:Adrenergic alpha-2 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D011758:Pyrroles; D010883:Piperoxan; C065161:fluparoxan