Zhou Qianghui, Gui Jinghan, Pan Chung-Mao, Albone Earl, Cheng Xin, Suh Edward M, Grasso Luigi, Ishihara Yoshihiro, Baran Phil S
Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
J Am Chem Soc. 2013 Sep 4;135(35):12994-7. doi: 10.1021/ja407739y. Epub 2013 Aug 22.
A general C-H functionalization method for the tagging of natural products and pharmaceuticals is described. An azide-containing sulfinate reagent allows the appendage of azidoalkyl chains onto heteroaromatics, the product of which can then be attached to a monoclonal antibody by a "click" reaction. This strategy expands the breadth of bioactive small molecules that can be linked to macromolecules in a manner that is beyond the scope of existing methods in bioconjugation to permit tagging of the "seemingly untaggable".
本文描述了一种用于天然产物和药物标记的通用C-H官能化方法。一种含叠氮化物的亚磺酸盐试剂可将叠氮烷基链连接到杂环芳烃上，其产物随后可通过“点击”反应连接到单克隆抗体上。这种策略扩展了生物活性小分子的范围，这些小分子能够以一种超出生物共轭现有方法范围的方式与大分子相连，从而实现对“看似无法标记的”物质进行标记。
