4.7 Article

Direct amidation of unprotected amino acids using B(OCH2CF3)(3)

期刊

CHEMICAL COMMUNICATIONS
卷 52, 期 57, 页码 8846-8849

出版社

ROYAL SOC CHEMISTRY
DOI: 10.1039/c6cc05147b

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资金

  1. Engineering and Physical Sciences Research Council (EPSRC) [EP/E052789/1]
  2. Department of Chemistry, University College London
  3. Pfizer (EPSRC CASE award)
  4. GlaxoSmithKline
  5. EPSRC [EP/E052789/1] Funding Source: UKRI
  6. Engineering and Physical Sciences Research Council [EP/E052789/1, 1353678] Funding Source: researchfish

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A commercially available borate ester, B(OCH2CF3)(3), can be used to achieve protecting-group free direct amidation of alpha-amino acids with a range of amines in cyclopentyl methyl ether. The method can be applied to the synthesis of medicinally relevant compounds, and can be scaled up to obtain gram quantities of products.

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