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【答案】应助回帖
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烟云听雨(金币+10, 翻译EPI+1): 谢谢 2011-06-25 10:55:42
Mally89(金币+1): 感谢应助！~ 2011-06-25 22:08:24
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The practical pursuit of such an approach presupposes efficient synthetic access to the desired scaffold, a prerequisite that might not be as straightforward as using the natural product itself as starting material. 这种方法实现的先决条件是有有效的合成所需支架的途径，这可能不像使用天然产物自身作为起始物料那样简单。An attractive alternative is to build the proposed scaffold de novo, an activity that can be considerably informed by knowledge gained in natural products total synthesis [i.e., the “diverted chemical synthesis” concept elucidated by Wilson and Danishefsky (10)]. 一种有吸引力的替代就是借鉴天然产物全合成信息从头合成所需的支架。In this paper, we describe the use of such a strategy to identify several potent sigma receptor(Sig-R) ligands. 本文中，我们描述使用这一策略鉴定几种Sig-R 受体的强力配体。The two key components of success were (i) efficient access to the lead natural products via total synthesis and (ii) the subsequent development of general synthetic methodology that allowed for systematic and flexible chemical optimization of a core moiety.两个成功的关键是：通过全合成得到先导天然产物的有效途径；随后建立整体合成方法以对核心部分进行系统化和灵活的化学优化。 |
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