A two-step, one-pot synthesis of diverse N-pyruvoyl amino acid derivatives using the Ugi reaction.

M Nakamura, J Inoue, T Yamada

Kobe Creative Center, Research Division of Senju Pharmaceutical Co., Ltd, Japan. masayuki-nakamura@senju.co.jp

Bioorganic & medicinal chemistry letters 2000 Dec 18

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A 100-member combinatorial library of alpha-ketoamides, which was designed to search potent cysteine protease inhibitors, was generated by a parallel solution-phase synthesis. A two-step one-pot synthesis, in which the Ugi reaction followed by pyridinium dichromate (PDC) oxidation was employed in the same reaction vessel, easily afforded the alpha-ketoamides in a short time.

Citation

M Nakamura, J Inoue, T Yamada. A two-step, one-pot synthesis of diverse N-pyruvoyl amino acid derivatives using the Ugi reaction. Bioorganic & medicinal chemistry letters. 2000 Dec 18;10(24):2807-10