Three-ingredient reaction system synthetic method of quinoline derivative

The present invention relates to synthetic method of a quinoline derivative shown as a formula (IV). The method comprises a cyclization reaction of a compound shown as a formula (I), a compound shown as a formula (II) and a compound shown as a formula (III) in an oxygen atmosphere and in the presenc...

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Bibliographic Details
Main Author LI GONGYUAN
Format Patent
LanguageEnglish
Published 28.10.2015
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The present invention relates to synthetic method of a quinoline derivative shown as a formula (IV). The method comprises a cyclization reaction of a compound shown as a formula (I), a compound shown as a formula (II) and a compound shown as a formula (III) in an oxygen atmosphere and in the presence of a catalyst, an activator and a nitrogen-containing ligand, so as to obtain the compound shown as formula (IV). R1 and R2 are each independently selected from H, C1-C6 alkyl, C1-C6 alkoxy and halogen; and X is halogen. The method uses comprehensive selection of catalyst, activator, nitrogen-containing ligand and solvent to play a unique synergic effect, which can get a high yield of the desired product; and the invention has good potential and industrialization prospect for application in the field of pharmaceutical intermediate synthesis.
Bibliography:Application Number: CN201510373794