Practical Synthesis of Unsymmetrical Ureas from Isopropenyl Carbamates

  • 10.1021/jo0507643
  • The Journal of Organic Chemistry
  • p 6960-6963, Volume 70, Issue 17,
  • journal-article
A very convenient method for the synthesis of unsymmetrical ureas is described, based on isopropenyl carbamates. The synthetic efficiency of traditional methods for urea formation, such as use of phosgene or alkyl and aryl carbamates, is limited by the formation of symmetrical urea side products or reaction reversibility. Isopropenyl carbamates react with amines cleanly and irreversibly and give unsymmetrical ureas in high yield and purity. This method is ideal for the rapid synthesis of compound libraries.

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Mild, High Yielding Method

Ureas are very widely used synthetic targets in pharmaceutical industry especially as kinase inhibitors. Using this methodology we have synthesized thousands of unsymmetrical ureas as kinase inhibitors. This method is a very mild, high yielding and can work for different...
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