187655-75-0Relevant academic research and scientific papers
Transient Directing Group Strategy as a Unified Method for Site Selective Direct C4-H Halogenation of Indoles
Kuang, Guanghua,Liu, Dandan,Chen, Xuerong,Liu, Guangyuan,Fu, Yang,Peng, Yiyuan,Li, Hua,Zhou, Yirong
supporting information, p. 8402 - 8406 (2021/11/13)
A unified method for direct C4-H halogenation of indoles has been accomplished with the assistance of anthranilic acids as suitable transient directing groups. Exclusive site selectivity (one out of five potential reactive sites) as well as good functional group tolerance was obtained to install three kinds of halogen atoms (Cl, Br and I, respectively) by using inexpensive N-halosuccinimides (NXS) as halogen sources under mild conditions. Taking advantage of the rich functional groups in the product, a diversity of nitrogen-containing heterocycles were facily constructed via one-step late-stage derivations.
4-position iodo indole compound and preparation method thereof (by machine translation)
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Paragraph 0048-0052; 0061-0064, (2020/12/15)
4-position iodoindole compounds and a preparation method thereof are disclosed. -3 -iodo indole compounds are prepared using various N -protected indole 4 formaldehyde and N - iodosuccinimide (NIS) as reaction substrates. The reaction yield can reach moderate to excellent, the chemical selectivity and the regional selectivity of the reaction are excellent, the reaction conditions are mild, and the application range of the substrate is wide. The operation is simple and convenient. The method is low in cost, less in side reaction, high in product purity, convenient to separate and purify and suitable for large-scale preparation, so that the obtained product has a very good application prospect in the field of biomedicine. (by machine translation)
A convenient preparation of 4-iodoindoles from indoles: Application to the chemical synthesis of hapalindole alkaloids
Brown, Martyn A.,Kerr, Michael A.
, p. 983 - 985 (2007/10/03)
4-Iodoindoles were synthesized via regioselective chloromercuration and subsequent iodination of a series of N-p-toluenesulfonyl indoles bearing a variety of substituents at the 3-position. This procedure allows rapid access to 3,4-dihaloindoles which may be used as synthetic precursors to indole alkaloids.
