Late-Stage Diversification of Biologically Active Molecules via Chemoenzymatic C-H Functionalization.
Late-Stage Diversification of Biologically Active Molecules via Chemoenzymatic C-H Functionalization.
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DOI：
10.1021/acscatal.5b02558
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发表时间：
2016-03-04
期刊：
影响因子：
12.9
通讯作者：
Lewis JC
中科院分区：
文献类型：
--
作者：
Durak LJ;Payne JT;Lewis JC
瑞贝卡霉素卤化酶的工程变体用于选择性卤化许多生物活性芳香族化合物。随后的Pd催化的交叉偶联反应的粗提取物上的这些反应被用来安装芳基，胺，和醚取代基的卤化位点。这种简单的化学酶促方法能够使一系列底物上的C-H键非定向官能化，以获得通过其他方法制备具有挑战性或效率低下的衍生物。
Engineered variants of rebeccamycin halogenase were used to selectively halogenate a number of biologically active aromatic compounds. Subsequent Pd-catalyzed cross-coupling reactions on the crude extracts of these reactions were used to install aryl, amine, and ether substituents at the halogenation site. This simple, chemoenzymatic method enables non-directed functionalization of C-H bonds on a range of substrates to provide access to derivatives that would be challenging or inefficient to prepare by other means.