PREPARATION OF ENYLMETHYLOXYCARBONYL-ASPARAGINE-PENTAFLUOROPHENYL ESTER FROM THE FREE ACID

Citation
Ji. Gyi et al., PREPARATION OF ENYLMETHYLOXYCARBONYL-ASPARAGINE-PENTAFLUOROPHENYL ESTER FROM THE FREE ACID, Synlett, (2), 1995, pp. 205-206
Citations number
6
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
ISSN journal
09365214
Issue
2
Year of publication
1995
Pages
205 - 206
Database
ISI
SICI code
0936-5214(1995):2<205:POEE>2.0.ZU;2-1
Abstract
We report a new method for synthesising Fmoc-asparagine pentafluorophe nyl ester from the free acid which is suitable for use directly in pep tide assemblies. The coupling reagent 1-(3-dimethylaminopropyl)-3-ethy lcarbodi-imide hydrochloride (EDC) is found to be highly effective for activating non-sidechain protected asparagine and it facilitates an e fficient water-based work-up. Yields of product are typically in the r ange of 65-75%.