Synthesis of novel 5-alkyl/aryl/heteroaryl substituted diethyl 3,4-dihydro-2H-pyrrole-4,4-dicarboxylates by aziridine ring expansion of 2-[(aziridin-1-yl)-1-alkyl/aryl/heteroaryl-methylene]malonic acid diethyl esters
2011

Synthesis of Novel Pyrrole Derivatives

publication Evidence: moderate

Author Information

Author(s): Satish S. More, Mohan T. Krishna, Kumar Y. Sateesh, Kumar U. K. Syam, Patel Navin B, Sibi Mukund P

Primary Institution: Dr. Reddy's Laboratories Ltd.

Hypothesis

Can iodide ion mediated ring expansion of N-vinylaziridines yield novel pyrrole derivatives?

Conclusion

The study successfully demonstrated the synthesis of novel 5-alkyl/aryl/heteroaryl substituted diethyl 3,4-dihydro-2H-pyrrole-4,4-dicarboxylates using iodide ion mediated aziridine ring expansion.

Supporting Evidence

  • The methodology yielded pyrrole derivatives in very good to excellent yields (81–93%).
  • Electron withdrawing groups on aryl rings slowed the reaction rates.
  • Various novel pyrroline derivatives were synthesized as key intermediates.

Takeaway

Scientists found a new way to make special chemical compounds called pyrroles, which can be used to create other important substances.

Methodology

The synthesis involved iodide ion mediated ring expansion of N-vinylaziridines under mild conditions to produce pyrrole derivatives.

Limitations

The reaction rates were slower for aryl substitutions compared to alkyl substitutions due to steric hindrance.

Digital Object Identifier (DOI)

10.3762/bjoc.7.95

Want to read the original?

Access the complete publication on the publisher's website

View Original Publication