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Cu一催化的不对称串联反应研究取得重要进展
含有多个连续手性中心的结构单元常见于各类天然产物和手性药物中,其合成一直是有机合成化学最具挑战的课题之一。在非环状的结构单元中高选择性地构造三个以上这样的连续多手性中心,其挑战性更大。发展高效的不对称催化方法是制备这类化合物的有效方法之一。
在中科院百人计划和国家自然科学基金的支持下,中国科学院兰州化学物理研究所炭基合成与选择氧化国家重点实验室夏春谷、黄汉民研究小组与浙江工业大学胡信全教授合作,利用亚胺能捕提在不对称Michael加成反应中原位形成手性烯醇活性中间体的特性,巧妙设计了一类高效不对称串联反应。
采用简单易得的α,β-不饱和酮、亚胺、烷基锋为原料,手性铜络合物为催化剂,通过串联反应方式一步就可以高立体选择性的合成具有三个连续非环状手性中心氮基酮类化合物。该方法已被成功应用于高选择性合成具有重要生理活性的多手性中心异吲噪啉酮和具有抗流感活性的多手性中心氮杂环丁烷。
(摘自中国科学院网站)