1-氧代-5-羟基色胺：一种出人意料的强效5-HT3（血清素）受体激动剂。
1-Oxo-5-hydroxytryptamine: a surprisingly potent agonist of the 5-HT3 (serotonin) receptor.
作者信息
Kedrowski Sean M A, Bower Kiowa S, Dougherty Dennis A
机构信息
Division of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, California 91125, USA.
出版信息
Org Lett. 2007 Aug 16;9(17):3205-7. doi: 10.1021/ol071083s. Epub 2007 Jul 18.
A novel synthetic route to 1-oxo-5-hydroxytryptamine, the benzofuran analogue of serotonin, has been developed. The new synthesis proceeds via the [3+2] cycloaddition of p-benzoquinone and 2,3-dihydrofuran, followed by a Lewis acid-catalyzed isomerization. This molecule proves to be a competent agonist (equipotent to serotonin) of the 5-HT3 receptor, demonstrating that the indolic proton of serotonin is not essential to its activation of the receptor.
已开发出一种合成1-氧代-5-羟基色胺（血清素的苯并呋喃类似物）的新路线。新合成方法是通过对苯醌与2,3-二氢呋喃的[3+2]环加成反应，然后进行路易斯酸催化的异构化反应。该分子被证明是5-HT3受体的有效激动剂（与血清素等效），这表明血清素的吲哚质子对其激活该受体并非必不可少。
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