Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 10, Issue 48, Pages 9538-9555Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob26498f
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The development of new practical and green methods for the synthesis of small heterocycles is an attractive area of research due to the well-known potential of heterocyclic small molecule scaffolds in the drug discovery process. Herein we report a one-pot, three-component sequential procedure for the synthesis of diversely 1,3,5- and 1,3,5,5-substituted hydantoins, in high yields and very mild conditions, using readily accessible starting materials such as azides, iso(thio)cyanates and substituted alpha-halo-acetic carboxylic acids. This methodology is especially convenient for the synthesis of spiro-hydantoins, which are particularly interesting bioactive compounds in medicinal chemistry.
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