Traceless solid-phase synthesis of mappicine ketone library via multiple chemoselective palladium-catalyzed reactions on benzenesulfonate linker.

[摘要]：We report here a solid-phase synthesis of a library of mappicine ketone (I) a leading antiviral compd. with activity against herpes viruses and human cytomegalovirus. The synthesis is based on multiple chemoselective palladium-catalyzed reactions involving a regioselective intramol. Heck reaction at C-2, substitution of Cl at C-7 by Suzuki-Miyaura cross-coupling reaction and Buchwald-Hartwig amination, and reductive cleavage of the benzenesulfonate linker at C-10.

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