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三氮烯合成子法构建螺环杂环化合物。

Trianion synthon approach to spirocyclic heterocycles.

机构信息

Department of Chemistry, 1102 Natural Sciences II, University of California, Irvine, Irvine, California 92697, United States.

出版信息

Org Lett. 2013 May 3;15(9):2226-9. doi: 10.1021/ol400788q. Epub 2013 Apr 17.

Abstract

A variety of spirocyclic heterocycles have been constructed by a double-alkylation and reductive cyclization approach utilizing α-heteroatom nitriles as trianion synthons. The method provides access to heteroatom-substituted spirocycles in a variety of ring sizes that are found in natural products and are important in pharmaceutical lead development and optimization.

摘要

利用α-杂原子腈作为三阴离子合成子,通过双烷基化和还原环化方法构建了各种螺环杂环。该方法可用于构建各种大小的杂原子取代的螺环,这些螺环存在于天然产物中,并且在药物先导化合物的开发和优化中非常重要。

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