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Althoughsyntheses of pelanserine (1) and goshuyuamide II (2) havebeen reported, there is still demand for more concise andefficient synthetic routes. In particular, no synthesis ofwuchuyuamide II (3) has been described thus far.Recently, we developed a new and useful methodology forthe one-step synthesis of a variety of quinazoline-2,4-dionesstarting from isatoic anhydride, primary amines, and triphos-gene in the presence of a base (Scheme 1).

Concise Synthesis of Pelanserine, Goshuyuamide II, and Wuchuyuamide II with Quinazolinedione Nuclei