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ky888

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The diversity oriented synthetic approach employed a threephase
approach called build/couple/pair (B/C/P). The first step –
the build phase – required the acquisition of stereochemically defined
building blocks with suitable functionality for coupling. The
building blocks were coupled to generate all possible stereoisomers,
and in the final pair phase, the linear precursors were intramolecularly
cyclised to give a diversity of ring systems. This
approach gave access to both medium-sized (8–9 atom) ring systems
and macrocycles with 12–14 atoms. As an illustration, all
stereoisomers of the building blocks 1 and 2 were generated (the
latter by stereocontrolled aldol condensations), and combined to
give all 8 stereoisomers of the dimer 3. Medium-sized rings (4)and macrocycles (5 and 6) were generated by nucleophilic aromatic
substitution, Huisgen [3 + 2] cycloaddition and ring-closing
metathesis (RCM) reactions.

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cluster8676

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ky888(金币+10, 翻译EPI+1): 很给力啊 谢谢啦 2011-07-02 01:58:37
Mally89(金币+2): 感谢应助!~欢迎常来!~ 2011-07-04 16:50:14
多样性导向的合成方法引入了三相方法称为构建/耦合/配对(B / C / P)。第一步,构建阶段 - 需要获得立体化学定义的并有合适的耦合功能的构建单元构建单元被耦合生成所有可能的立体异构体,在最后配对阶段,线性前体分子内成环生成不同的环系统。这种方法既能获得了中型(8-9原子)环系统,还能获得大环化合物(12-14原子)。作为一个例证,构建单元1和2的所有立体异构体均可被合成(后者来自立体选择性羟醛聚合),他们互相结合又能生成所有8个二聚体3的立体异构体。中型环(4)和大环(5和6)是由亲核芳香取代,Huisgen [3 2]环加成反应和环闭合复分解(RCM)反应而生成的。
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