method for the preparation of N,3-disubstituted indoles and 3-hydroxyl indolines. This synthetic strategy relies on an epoxide-opening followed by an intramolecular SNAr of the resulting fluoroaryl amino alcohols. The reaction afforded 3-hydroxyl indolines when carried out at lower temperature for the derivatives bearing multi-fluorine substituents at the aromatic ring.
在这封信中,我们描述了一种实用且用途广泛的方法,用于制备N,3-二取代的
吲哚和3-羟基二氢
吲哚。此合成策略依赖于
环氧化物的开口,随后通过分子内小号Ñ所得
氟化芳基
氨基醇的
氩气。当在较低温度下进行时,对于在芳环上带有多
氟取代基的衍
生物,该反应提供了3-羟基二氢
吲哚。