作者:Parul Pal、Meghan Fragis、Jakob Magolan、Srinivas Dharavath、Jarrod W. Johnson
DOI:10.1055/a-1868-4148
日期:2022.11
Fischer indole reactions. These vinyl sulfides react with arylhydrazines in the presence of TsOH·H2O in refluxing ethanol or dichloroethane to yield diverse 3-substituted and 2,3-disubstituted indoles or azaindoles. The utility of this chemistry is highlighted with the efficient preparation of three biomedically relevant compounds: 4-aza-melatonin, a furoindoline, and an indomethacin-like CRTh2 antagonist
使用硫代烷基鏻盐通过 Wittig 烯化获得的乙烯基硫化物在 Fischer 吲哚反应中用作醛或酮替代物。这些乙烯基硫化物在 TsOH·H 2 O 存在下,在回流的乙醇或二氯乙烷中与芳基肼反应,生成不同的 3-取代和 2,3-二取代吲哚或氮杂吲哚。通过有效制备三种生物医学相关化合物,突出了该化学的实用性:4-氮杂-褪黑激素、呋喃二氢吲哚和吲哚美辛样 CRTh2 拮抗剂。