4.7 Article

Room temperature ICl-induced dehydration/iodination of 1-acyl-5-hydroxy-4,5-dihydro-1H-pyrazoles.: A selective route to substituted 1-acyl-4-iodo-1H-pyrazoles

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 73, Issue 17, Pages 6666-6670

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jo800789p

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Funding

  1. National Institute of General Medical Sciences [R01 GM070620, R01 GM079593]
  2. National Institutes of Health Kansas University Center of Excellence [P50 GM069663]

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A number of new functionally substituted 1-acyl-5-hydroxy-4,5-dihydro-1H-pyrazoles have been prepared in moderate to excellent yields from the corresponding 2-alkyn-1-ones. The resulting dihydropyrazoles undergo dehydration and iodination in the presence of 10 and Li(2)CO(3) at room temperature to provide 1-acyl-4-iodo-1H-pyrazoles.

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