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An efficient synthetic protocol for amide derivatives of Boc-2-aminoisobutyrate
- Issue Date
- Mar-2018
- Publisher
- PHARMACEUTICAL SOC KOREA
- Keywords
- Transmidation; t-butylmagnesiumchloride; Steric challenge; Methyl Boc-aminoisobutyrate
- Citation
- ARCHIVES OF PHARMACAL RESEARCH, v.41, no.3, pp.259 - 264
- Indexed
- SCIE
SCOPUS
KCI
- Journal Title
- ARCHIVES OF PHARMACAL RESEARCH
- Volume
- 41
- Number
- 3
- Start Page
- 259
- End Page
- 264
- ISSN
- 0253-6269
- Abstract
- Aminoisobutyric acid (AIB) is an important building block widely incorporated by medicinal chemists in molecular design. Owing to the steric challenge, elaborating AIB's carboxylic acid using conventional amidation protocols is often problematic. We discovered that an amidation protocol utilizing methyl Boc-aminoisobutyrate and magnesium amidates of various reactivities produces the corresponding amide derivatives in good to excellent yields. [GRAPHICS] .
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