通过 PhIO 促进的α-吲哚基腙的分子内氧化环化合成氮杂咔啉。
Synthesis of Azacarbolines via PhIO-Promoted Intramolecular Oxidative Cyclization of α-Indolylhydrazones.
机构信息
Department of Biomolecular Sciences, Section of Chemistry and Pharmaceutical Technologies, University of Urbino "Carlo Bo", Via I Maggetti 24, 61029 Urbino, Italy.
出版信息
J Org Chem. 2021 Dec 17;86(24):17918-17929. doi: 10.1021/acs.joc.1c02217. Epub 2021 Dec 6.
Abstract
An unprecedented synthesis of polysubstituted indole-fused pyridazines (azacarbolines) from α-indolylhydrazones under oxidative conditions using a combination of iodylbenzene (PhIO) and trifluoroacetic acid (TFA) has been developed. This transformation is conducted without the need for transition metals, harsh conditions, or an inert atmosphere.
摘要
一种前所未有的在氧化条件下，通过碘苯（PhIO）和三氟乙酸（TFA）的组合，从α-吲哚腙合成多取代吲哚并哒嗪（氮杂咔啉）的方法已经被开发出来。这种转化不需要过渡金属、苛刻的条件或惰性气氛。
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