Practical one-pot amidation of N-Alloc-, N-Boc-, and N-Cbz protected amines under mild conditionsopen access
- Authors
- Van Hieu Tran; Kim, Hee-Kwon; Hong, Wan Pyo
- Issue Date
- May-2021
- Publisher
- ROYAL SOC CHEMISTRY
- Citation
- RSC ADVANCES, v.11, no.26, pp.15890 - 15895
- Journal Title
- RSC ADVANCES
- Volume
- 11
- Number
- 26
- Start Page
- 15890
- End Page
- 15895
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/84584
- DOI
- 10.1039/d1ra02242c
- ISSN
- 2046-2069
- Abstract
- A facile one-pot synthesis of amides from N-Alloc-, N-Boc-, and N-Cbz-protected amines has been described. The reactions involve the use of isocyanate intermediates, which are generated in situ in the presence of 2-chloropyridine and trifluoromethanesulfonyl anhydride, to react with Grignard reagents to produce the corresponding amides. Using this reaction protocol, a variety of N-Alloc-, N-Boc-, and N-Cbz-protected aliphatic amines and aryl amines were efficiently converted to amides with high yields. This method is highly effective for the synthesis of amides and offers a promising approach for facile amidation.
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