2-Fluoroalkyl-substituted indoles were prepared in moderate to excellent yields through bromotriphenylphosphonium salt promoted ring formation with fluorine-containing carboxylic acids in the presence of triethylamine in toluene at reflux temperature. A range of 2-fluoroalkyl-substituted indole derivatives can be conveniently prepared.
A new simple and efficient one‐pot synthesis of 2‐fluoroalkyl substituted indoles from 2‐aminobenzyl alcohols with fluorine‐containing carboxylic acids in the presence of Ph3P, CCl4, and NEt3 is described. Various kinds of 2‐fluoroalkyl substituted indole derivatives can be conveniently prepared.
Two types of fused pyrimidones, 3-substituted-7-chloro-4H-pyrimido[1,2-b]pyridazin-4-ones and 6-substituted-5H-thiazolo-[3,2-a]pyrimidin-5-ones were easily prepared from Baylis-Hillman adduct acetates under microwave irritation in high yields.
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