Houlden Chris E, Bailey Chris D, Ford J Gair, Gagné Michel R, Lloyd-Jones Guy C, Booker-Milburn Kevin I
School of Chemistry, Cantock's Close, University of Bristol, Bristol, BS8 1TS, UK.
J Am Chem Soc. 2008 Aug 6;130(31):10066-7. doi: 10.1021/ja803397y. Epub 2008 Jul 10.
A Pd-catalyzed intermolecular 1,2-carboamination route to indolines from N-aryl ureas and 1,3-dienes that proceeds under mild conditions in relatively nonacidic media, is presented. The in situ generation, or preformation, of a palladium tosylate emerges as a key parameter in gaining the requisite reactivity for the C-H insertion/carbopalladation/nucleophilic displacement process.
本文介绍了一种钯催化的分子间1,2-碳胺化反应路线,该路线可在温和条件下于相对非酸性介质中由N-芳基脲和1,3-二烯制备二氢吲哚。对甲苯磺酸钯的原位生成或预形成是实现C-H插入/碳钯化/亲核取代过程所需反应活性的关键参数。