5463-89-8Relevant academic research and scientific papers
2-aryl-3-acylamino quinoline derivative and preparation method thereof
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, (2017/12/09)
The invention provides a 2-aryl-3-acylamino quinoline derivative and a preparation method thereof. The method includes the steps of: taking 2-Boc-aminobenzaldehyde as the raw material, carrying out condensation reaction with substituted acetophenone under an alkaline condition to obtain a chalcone derivative, then conducting cyclization by an amination reagent to obtain substituted cyclopropylamine, reacting the product with acyl chloride, and finally under an acidic condition, conducting deprotection and ring formation simultaneously, thus obtaining the 2-aryl-3-acylamino quinoline derivative. The invention adopts a one-pot process, while the protecting group is removed, and ring closing reaction is carried out on the cyclopropylamine intermediate in an acidic aqueous solution directly to obtain the 2-aryl-3-acylamino quinoline derivative. The method has the advantages of mild reaction conditions and simple steps, etc., and has no need for high temperature, strong alkali or other harsh conditions.
