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5-Methoxypiperonal is used in the synthesis of oxazole combretastatin A-4 analogs showing anti-tumor activity. It is also used in the synthesis of endothelin-A antagonist ABT-546, and further in the synthesis of antidepressant rolipram.
David M. Barnes; Jianguo Ji; Michael G. Fickes; Michael A. Fitzgerald; Steven A. King; Howard E. Morton; Frederick A. Plagge; Margo Preskill; Seble H. Wagaw; Steven J. Wittenberger and Ji Zhang. Development of a Catalytic Enantioselective Conjugate Addition of 1,3-Dicarbonyl Compounds to Nitroalkenes for the Synthesis of Endothelin-A Antagonist ABT-546. Scope, Mechanism, and Further Application to the Synthesis of the Antidepressant Rolipram. J. Am. Chem. Soc. 2002, 124 (44), 13097-13105.