Novel Synthesis of 4-Substituted Pyridine-2,6-Dicarboxylic Acid Derivatives (No. 0071)

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4-Substituted pyridine-2,6-dicarboxilic acids and their derivatives are important building blocks in the synthesis of bioactive molecules, chemical probes for biological research, solid-supported reagents and other functional molecules. However, known methods for the synthesis of 4-substituted pyridine-2,6-dicarboxylic acids derivatives often require long synthetic routes and harsh conditions. A team of OIST researchers led by Prof. Fujie Tanaka has developed a new synthetic protocol that overcomes the above problems and provides a simple one-pot method to unlock new derivatives.


Lead Researcher:
Fujie Tanaka

Faculty of Chemistry and Chemical Bioengineering Unit


  • Therapeutic and preventative medicine
  • Drug development
  • Chemical probes for biological research



  • Mild conditions
  • One-pot reaction
  • High atom economy

The dihydro-2H-pyran precursor (1) can be readily synthesized in the same pot from aldehydes and pyruvates, which is also an OIST invention (OIST ref. 0023).

The OIST team built a library of novel 4-substituted pyridine-2,6-carboxylic acid derivatives

Click on the images to enlarge



This is a novel method to synthesize chemically and biologically important 4-substituted pyridine-2,6-dicarboxylic acid derivatives, whereby pyruvates and aldehydes are reacted with a pyrrolidine-acetic acid catalyst to form dihydropyran derivatives, which are further reacted with ammonium acetate in one pot under mild conditions to yield the desired products.


Media Coverage and Presentations



  Paola Butler-Zanetti
Technology Licensing Section