First synthesis of thiazepino[3,4‐a]isoquinolines, a facile new synthetic route to diazepino[3,4‐a]isoquinolines and assessment of their dopamine and σ receptor affinities,Journal of Heterocyclic Chemistry

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First synthesis of thiazepino[3,4‐a]isoquinolines, a facile new synthetic route to diazepino[3,4‐a]isoquinolines and assessment of their dopamine and σ receptor affinities
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-07-04 , DOI: 10.1002/jhet.4086
Pierpaolo Cordone _{1,

2} , Hari Krishna Namballa ₁ , Wayne Wesley Harding _{1,

2,

3}

Affiliation

Heterocycles that bear the novel 5,6,14,14a‐tetrahydro‐8H‐benzo[6,7][1,4]thiazepino[3,4‐a]isoquinoline and the 5,6,14,14a‐tetrahydro‐8H‐13l2‐benzo[6,7][1,4]diazepino[3,4‐a]isoquinoline frameworks were synthesized in a facile manner. These tetrahydroprotoberberine (THPB)‐inspired scaffolds demonstrate selective affinity for the σ₁R in contrast to the naturally occurring THPB congeners that show D₁R and σ₂R selectivity.

中文翻译：

首次合成硫氮杂[3,4-a]异喹啉，一种简便的合成地氮杂[3,4-a]异喹啉的新途径及其多巴胺和σ受体亲和力的评估

带有新型 5,6,14,14a-四氢-8H-苯并[6,7][1,4]thiazepino[3,4-a]isoquinoline 和 5,6,14,14a-四氢-8H 的杂环‐13l2-苯并[6,7][1,4]二氮杂[3,4-a]异喹啉骨架以简便的方式合成。与显示 D ₁ R 和 σ ₂ R 选择性的天然 THPB 同源物相比，这些受四氢原小檗碱 (THPB) 启发的支架显示出对 σ ₁ R 的选择性亲和力。

更新日期：2020-07-04

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