钯催化通过降冰片烯介导的区域选择性级联 C-H 活化实现吲哚的直接 2-烷基化反应。
Palladium-catalyzed direct 2-alkylation of indoles by norbornene-mediated regioselective cascade C-H activation.
机构信息
Lehrstuhl für Organische Chemie I and Catalysis Research Center (CRC), Technische Universität München, Lichtenbergstrasse 4, 85747 Garching, Germany.
出版信息
J Am Chem Soc. 2011 Aug 24;133(33):12990-3. doi: 10.1021/ja2055066. Epub 2011 Aug 2.
PMID:21806073
Abstract
A palladium-catalyzed direct 2-alkylation reaction of free N-H indoles has been developed. This reaction relies on a norbornene-mediated cascade C-H activation process at the indole ring, which features high regioselectivity and excellent functional group tolerance. The reaction represents the first example for a generally applicable, direct C-H alkylation of indole at the 2-position.
摘要
钯催化的游离 N-H 吲哚的直接 2-烷基化反应已经被开发出来。该反应依赖于降冰片烯介导的吲哚环级联 C-H 活化过程，具有高区域选择性和优异的官能团耐受性。该反应代表了首例普遍适用的、吲哚 2-位直接 C-H 烷基化反应的例子。
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