An efficient synthetic protocol for amide derivatives of Boc-2-aminoisobutyrate
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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.
KeywordsMethyl Boc-aminoisobutyrate Transmidation t-butylmagnesiumchloride Steric challenge
This research was supported by the Basic Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (NRF-2015R1A2A2A04003471).
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Conflict of Interest
The authors declare no conflict of interest
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