Abstract

A new four-component 1,4-diketopiperazine formation is described via an Ugi/Pictet-Spengler two-step procedure. The use of α-ketocarboxylic acids and homoveratryl isocyanide allows the formation of α-keto amides along with cyclised 6-hydroxypiperazines. The mixtures are not separated but directly treated with trifluoroactic acid to afford a tricyclic 2,5-diketopiperazine in a Pictet-Spengler-type cyclisation.

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