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烟云听雨(金币+10, 翻译EPI+1): 非常感谢 2011-07-21 09:00:56
Mally89(金币+1): 感谢应助!~ 2011-07-23 22:02:02
This observation permitted us to investigate an alternative Diels–Alder/aza–Wittig reaction sequence that afforded the tricyclic skeleton 9, which contained an unmasked basic nitrogen amenable to alkylation or amidation as desired (Scheme 3). 这一观察使得我们可以研究提供三环骨架9的可选Diels–Alder/aza–Wittig 反应序列,三环骨架9中含有未加修饰、易于按需进行烷基化或酰胺化的碱性氮。The scaffold readily participated in reductive amination with a diverse range of aldehydes to provide a collection of tertiary amines in this series. 支架使得多种多样的醛类易于发生还原氨化反应而得到一系列的叔胺。Given the precedent of diverse GPCR binding observed for the basic nitrogen-containing compounds previously profiled (see Figs. 3 and 4), we reasoned that this collection of compounds would afford interesting screening results. 基于先前研究的碱性含氮化合物各异的GPCR亲和性先例,我们推理此系列化合物应该具有不错的筛选结果。We were inclined toward screening against the opioid receptors and Sig-Rs based on the association of these receptors with antitussive activity (40, 41), and we began our profiling investigations with these. 我们倾向于针对阿片受体和与镇咳活性相关的Sig-R进行筛选,我们已经开始有关的横断面研究。
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