Abstract
Synthesis of Nα-protected amino/peptide Weinreb amides employing N,N'-carbonyldiimidazole as activating agent; studies on docking and antibacterial activities
Highlights
Weinreb amides have wide importance in organic synthesis due to their versatile reactivity with nucleophiles and selective reduction to aldehydes
Chemistry: For the synthesis of the Nα-protected Weinreb amides (2a-2m), Nα-protected amino acid was dissolved in THF; CDI was added at 0° C and the solution was stirred for about 10 min
The carboxylic group of amino acids was activated using CDI followed by the coupling reaction with N, O- dimethyl hydroxylamine hydrochloride salt to obtain the title products
Summary
Weinreb amides have wide importance in organic synthesis due to their versatile reactivity with nucleophiles and selective reduction to aldehydes. We report an efficient, one pot synthesis of Nα-protected amino acid/peptide acid-derived Weinreb amides employing CDI as activating agent. In this way several Weinreb amides were synthesized from Nα-protected Fmoc/Cbz/Boc amino acids (Table 1).
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