A Conventional New Procedure for N-Acylation of Unprotected Amino Acids
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概要
- 論文の詳細を見る
The preparation of amide derivatives (4) by N-acylation of unprotected α-amino acids is easily achieved via readily available benzotriazolyl carboxylates (2a-d) or succinimidyl carboxylates (2e-f). These intermediates (2) are prepared from reaction of carboxylic acids (1) with 1-hydroxybenzotriazole (HO-Bt) or N-hydroxysuccinimide (HO-Su) in the presence of equimolar amounts of 1-ethyl-3-(3'-dimethylaminopropyl)carbodiimide hydrochloride (WSCI). The overall yields of the target compounds (4) were excellent, and this two-stage procedure could be applicable as an alternative procedure for one-pot reaction.
- 公益社団法人日本薬学会の論文
- 2007-01-01
著者
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Oishi Marumi
Faculty Of Pharmaceutical Sciences Fukuoka University
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Sumoto K
Faculty Of Pharmaceutical Sciences Fukuoka University
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Sumoto Kunihiro
Fukuoka Univ. Fukuoka Jpn
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Sumoto Kunihiro
Faculty Of Pharmaceutical Sciences Fukuoka University
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Fujisaki Fumiko
Faculty Of Pharmaceutical Sciences Fukuoka University
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Sumoto Kunihiro
Faculty of Pharmaceutical Science, Fukuoka University
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Fujisaki Fumiko
Faculty of Pharmaceutical Science, Fukuoka University
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