- Synthesis and application of a novel coupling reagent, ethyl 1-hydroxy- 1H-1,2,3-triazole-4-carboxylate
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An optimal coupling reagent, ethyl 1-hydroxy-1H-1,2,3-triazole-4- carboxylate (HOCt), has been designed and synthesised for application to solid phase peptide synthesis using Fmoc chemistry. It is used in combination with carbodiimide reagents, has very high coupling efficiency, and does not absorb at 302nm, thus allowing real-time monitoring of each coupling cycle. Its applications in the synthesis of endothelin analogues and difficult sequences are also discussed.
- Jiang, Lu,Davison, Amanda,Tennant, George,Ramage, Robert
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p. 14233 - 14254
(2007/10/03)
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- 40. Diazoaldehyde chemistry: Part 3. Synthesis of 4-acyl-1H-1,2,3-triazole derivatives
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Ten new α -diazo-β-oxoaldehydes were condensed with aniline, ammonia, hydroxylamine, and semicarbazide to yield new 4-acyl-(1-substituted)-1H-1,2,3-triazoles in moderate-to-good yields. The method is simple and regiospecific. The latter feature makes this method superior to the widely used acylacetylene + azide approach.
- Sezer, Oezkan,Dabak, Kadir,Akar, Ahmet,Anac, Olcay
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p. 449 - 453
(2007/10/03)
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