LAQV@REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa , Campus de Caparica, 2829-516 Caparica, Portugal.
Org Lett. 2016 Jul 1;18(13):3250-3. doi: 10.1021/acs.orglett.6b01500. Epub 2016 Jun 22.
A practical palladium-catalyzed cascade C-N cross-coupling/Heck reaction of alkenyl bromides with amino-o-bromopyridines is described for a straightforward synthesis of substituted 4-, 5-, 6-, and 7-azaindoles using a Pd2(dba)3/XPhos/t-BuONa system. This procedure consists of the first cascade C-N cross-coupling/Heck approach toward all four azaindole isomers from available aminopyridines. The scope of the reaction was investigated and several alkenyl bromides were used, allowing access to different substituted azaindoles. This protocol was further explored for N-substituted amino-o-bromopyridines.
描述了一种实用的钯催化的烯基溴化物与氨基-o-溴吡啶的串联 C-N 交叉偶联/Heck 反应，该反应采用 Pd2(dba)3/XPhos/t-BuONa 体系，用于通过直接合成取代的 4-、5-、6-和 7-氮杂吲哚。该方法由第一个串联 C-N 交叉偶联/Heck 方法构成，从可用的氨基吡啶中得到所有四种氮杂吲哚异构体。该反应的范围进行了研究，并使用了几种烯基溴化物，从而可以获得不同取代的氮杂吲哚。该方案进一步用于 N-取代的氨基-o-溴吡啶。
