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通过 In(OTf)3 催化的芳基碘化反应实现天然产物的温和衍生化。

Mild arming and derivatization of natural products via an In(OTf)3-catalyzed arene iodination.

机构信息

Department of Chemistry, P.O. Box 30012, Texas A&M University, College Station, Texas 77842-3012, USA.

出版信息

Org Lett. 2010 May 7;12(9):2104-7. doi: 10.1021/ol100587j.

Abstract

Iodination of arene-containing natural products employing N-iodosuccinimide catalyzed by In(OTf)(3) at ambient temperature is reported as a versatile and mild method for natural product derivatization amenable to small scale. This process facilitates natural product derivatization of arene moieties for SAR studies, homo- and heterodimerization of natural products, and also conjugation with reporters such as biotin via subsequent metal-mediated coupling reactions.

摘要

采用 N-碘代琥珀酰亚胺(N-iodosuccinimide)在三氟化铟(In(OTf)(3))催化下,室温下对含芳环的天然产物进行碘化反应,报道了一种通用且温和的天然产物衍生化方法,适用于小规模反应。该方法促进了芳环部分的天然产物衍生化,用于 SAR 研究、天然产物的同二聚和异二聚以及与生物素等报告分子的连接,通过后续的金属介导偶联反应。

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