A copper/iodine cocatalyzed decarboxylative cyclization of α-amino acids is described. Starting from the readily available amino acids and either 2-benzoylpyridines or 2-benzoylquinolines, 1,3-disubstituted imidazo[1,5-a]pyridines and 1,3-disubstituted imidazo[1,5-a]quinolines were prepared in excellent yields.
An electrochemically intramolecular functionalization of C(sp)-H bonds with masked oxygen nucleophiles was developed. With KI as the catalyst and electrolyte, diverse trisubstituted 2-oxazolines were constructed in good to excellent yields. This newly developed electrochemical dehydrogenative approach features external oxidant-free and additive-free conditions.
A highly diastereo- and enantioselective aziridination of N-sulphonyl ketimines with unfunctionalized ketones was reported. In this efficient method, a sequential direct asymmetric Mannich reaction and oxidative C-H amination were involved, which enabled a straightforward route to multisubstituted-fused aziridines in one pot. More importantly, two different products could be selectively obtained in the reaction by adding or removing a metal additive.
2‐Aryloylpyridines or quinolines efficiently react with aryl or alkyl substituted α‐amino acids, thus offering not only a novel approach to 1,3‐diaryl substituted imidazo[1,5‐a]pyridines, but also to 3‐alkyl‐1‐aryl substituted derivatives which are difficult to access by previously developed methods.
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