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The concise synthesis of the novel telomerase inhibitors dictyodendrins B and E was completed in only 9 and 11 steps (longest linear sequence). The highly convergent strategy employed a palladium-catalyzed Larock indole synthesis and a palladium-mediated one-pot consecutive Buchwald-Hartwig amination/C-H activation reaction as key steps. The present synthesis exhibits respectable levels of atom-, redox-, and step-economy.

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A full account of the concise total syntheses of dictyodendrins B and E, and the formal synthesis of dictyodendrin C are described. A palladium‐catalysed Larock indole synthesis was used to form the highly substituted indole core, and a palladium‐mediated one‐pot consecutive Buchwald–Hartwig amination/C–H activation reaction was used to construct the key pyrrolo[2,3‐c]carbazole core. Unsuccessful synthetic strategies are also discussed.

The rhodium(III)-catalyzed intramolecular annulation of alkyne-tethered acetanilides for the synthesis of fused tricyclic indole scaffolds via C-H activation has been developed, which has the potential for the synthesis of many indole alkaloids. This reaction proceeds under mild reaction conditions and with tolerance to a variety of functional groups.

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Dioxides. Part 8. Synthesis and Pharmacological Evaluation of Tricyclic Fused Quinazolines and 1,2,4-Benzothiadiazine 1,1-Dioxides as Potential α 1 -Adrenoceptor Antagonists.-A series of title compounds, e.g. (VI) and (IX)-(XII), is synthesized. Several products, such as (IXb) and (X), show high affinity for the α 1 -adrenoceptor, but compound (S)-(XI) and its hydrolysis product (XII) are the most highly selective and potent α 1 antagonists. -(CHERN, J.-W.; TAO, P.-L.; WANG, K.-C.; GUTCAIT, A.; LIU, S.-W.; YEN, M.-H.; CHIEN, S.-L.; RONG, J.-K.; J.