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通过 Pd 催化的 3-重氮吲哚啉-2-亚胺与芳基硼酸的偶联反应以及对 3-芳基-3-氟吲哚啉-2-亚胺的扩展来制备 2-氨基-3-芳基吲哚。

Preparation of 2-Amino-3-arylindoles via Pd-Catalyzed Coupling between 3-Diazoindolin-2-imines and Arylboronic Acids as well as Their Extension to 3-Aryl-3-fluoroindolin-2-imines.

出版信息

Org Lett. 2017 Sep 1;19(17):4604-4607. doi: 10.1021/acs.orglett.7b02211. Epub 2017 Aug 22.

Abstract

2-Amino-3-arylindoles were conveniently prepared from 3-diazoindolin-2-imines and arylboronic acids through palladium carbene intermediates in moderate to excellent yields. The synthesized 2-amino-3-arylindoles could be fluorinated with NFSI to afford 3-aryl-3-fluoroindolin-2-imines.

摘要

2-氨基-3-芳基吲哚可通过钯卡宾中间体从 3-重氮吲哚啉-2-亚胺和芳基硼酸方便地制备,产率中等至优秀。合成的 2-氨基-3-芳基吲哚可以用 NFSI 氟化得到 3-芳基-3-氟吲哚啉-2-亚胺。

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