Pfitzinger Reaction in the Synthesis of Bioactive Compounds - A Review
Jaiprakash N. Sangshetti,
Abhay S. Zambare,
Devanand B. Shinde.
Pfitzinger reaction is the formation of derivative of 4-quinoline carboxylic acids from isatins or its analogs under
alkaline condition. This reaction was first discovered by Pfitzinger at the end of 19th century hence it is known as
Pfitzinger reaction. This reaction has attracted a great deal of attention in the last few decades because of biological significance
of quinoline carboxylic acid derivatives. The utility of Pfitzinger reaction has been proved time to time by its involvement
in the synthesis of drugs or drug intermediates.
The present review is focused on brief aspects of the synthesis of 4-quinoline carboxylic acids from isatins and its different
derivatives. It also covers the literature on modification of original Pfitzinger reaction and its application for the synthesis
of different bioactive molecules.
Different 4-quinoline carboxylic acids analogs synthesized by Pfitzinger reaction or modified Pfitzinger reaction have
been tested for varied pharmacological activities. The review encompasses all literature reports of Pfitzinger reaction in
the synthesis of different pharmacologically active molecules. This reaction with some modification has been widely used
for the synthesis of a number of drugs or drug intermediates. The review also discusses the different chemistry aspects of
Keywords: Pfitzinger reaction, isatin derivatives, ketones, quinoline-4-carboxylic acid, bioactive molecules.
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