Convenient primary amidation of N-protected phenylglycine and dipeptides without racemization or epimerization |
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Authors: | Takuya Noguchi Seunghee JungNobuyuki Imai |
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Institution: | Faculty of Pharmacy, Chiba Institute of Science, 15-8 Shiomi-cho, Choshi, Chiba 288-0025, Japan |
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Abstract: | Primary amidation of N-protected phenylglycine and dipeptide proceeded easily to afford the corresponding amides in 57–95% yields with 99% ee and 81–99% de, respectively. The procedure is very easy to avoid racemization and epimerization of the products in the reactions by keeping exactly the reaction temperature at −15 °C when the activation of carboxylic acids, followed by the reaction of the mixed carbonic carboxylic anhydride with NH4Cl. |
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Keywords: | Phenylglycine Dipeptide Ethyl chloroformate Without racemization Without epimerization |
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