通过串联缩合/分子内硝酮-烯烃[3+2]环加成策略轻松获得富含sp(3)的杂环化学支架。
Facile access to a heterocyclic, sp(3)-rich chemical scaffold via a tandem condensation/intramolecular nitrone-alkene [3+2] cycloaddition strategy.
作者信息
Rawling M J, Storr T E, Bawazir W A, Cully S J, Lewis W, Makki M S I T, Strutt I R, Jones G, Hamza D, Stockman R A
机构信息
School of Chemistry, University of Nottingham, Nottingham, NG7 2RD, UK.
出版信息
Chem Commun (Camb). 2015 Aug 18;51(64):12867-70. doi: 10.1039/c5cc05070g.
PMID:26169627
Abstract
A heterocyclic, sp(3)-rich chemical scaffold was synthesised in just 6 steps via a highly regio- and diastereo-selective tandem nitrone formation/intramolecular nitrone-alkene [3+2] cycloaddition reaction. A library of 543 lead-like compounds based on the scaffold core has been produced.
摘要
通过高度区域和非对映选择性串联硝酮形成/分子内硝酮-烯烃[3+2]环加成反应，仅6步就合成了一种富含sp(3)的杂环化学支架。基于该支架核心已制备了一个包含543种类先导化合物的文库。
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