A domino N-amidoacylation/aldol-type condensation approach to the synthesis of the topo-I inhibitor Rosettacin and derivatives.

作者: Frédéric Pin , Sébastien Comesse , Morgane Sanselme , Adam Daïch

DOI: 10.1021/JO702387Q

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摘要: The pot, atom, and step-economic synthesis of Rosettacin topo-I poison its derivatives has been achieved using a novel domino N-amidoacylation/aldol-type condensation, followed by decarboxylation the ester function. key procedure simply involves mixing HOBt as new reagent with lactam NaH together in THF or THF/ DMF. reaction seems to be general led suitable N-heterocyclic products moderate good yields.

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