Expeditious Total Syntheses of Camptothecin and 10-Hydroxycamptothecin.

[摘要]：New expeditious total syntheses of (S)-camptothecin (16% overall yield, 95% ee) and (S)-10-hydroxycamptothecin (14% overall yield, 99% ee) have been accomplished, resp., starting from readily available and inexpensive materials. Development, optimization, and successful application of the cascade reaction consisting of a pyrrolidine-catalyzed Michael addn., an intramol. aldol condensation, and an oxidative aromatization, the intramol. oxa Diels-Alder cycloaddn., and the Sharpless asym. dihydroxylation make these two new syntheses more efficient and straightforward.

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