作为选择性α2-肾上腺素能受体拮抗剂的苯并二氧杂环吡咯的合成
Synthesis of benzodioxinopyrroles as selective alpha 2-adrenoceptor antagonists.
作者信息
Kitchin J, Borthwick A D, Brodie A C, Cherry P C, Crame A J, Pipe A J, Procopiou P A, Seaman M A, Turnbull J P
机构信息
Department of Medicinal Chemistry, Glaxo-Wellcome, Stevenage, Hertfordshire, UK.
出版信息
Bioorg Med Chem. 1995 Dec;3(12):1595-603. doi: 10.1016/0968-0896(95)00143-3.
PMID:8770384
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).
摘要
一系列新型四氢苯并二氧杂环吡咯已被鉴定为强效且选择性的α2-肾上腺素能受体拮抗剂。已开发出汇聚合成法，可用于制备类似物及其对映体。一种特别受关注的化合物是5-氟取代类似物（氟哌罗生）。
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