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A Conventional New Procedure for N-Acylation of Unprotected Amino Acids
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- Fujisaki Fumiko
- Faculty of Pharmaceutical Sciences, Fukuoka University
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- Oishi Marumi
- Faculty of Pharmaceutical Sciences, Fukuoka University
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- Sumoto Kunihiro
- Faculty of Pharmaceutical Sciences, Fukuoka University
Bibliographic Information
- Other Title
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- Conventional New Procedure for N Acylation of Unprotected Amino Acids
- A Conventional New Procedure for N‐Acylation of Unprotected Amino Acids.
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Description
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.
Journal
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- Chemical and Pharmaceutical Bulletin
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Chemical and Pharmaceutical Bulletin 55 (1), 124-127, 2007
The Pharmaceutical Society of Japan
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Keywords
Details 詳細情報について
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- CRID
- 1390001204170263936
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- NII Article ID
- 110006151447
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- NII Book ID
- AA00602100
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- ISSN
- 13475223
- 15222667
- 00092363
- 09317597
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- NDL BIB ID
- 8589042
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- PubMed
- 17202715
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL Search
- Crossref
- CiNii Articles
- OpenAIRE
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- Abstract License Flag
- Disallowed