化学選択的パラジウム触媒反応を利用したマッピシンケトン誘導体の固相合成研究

抄録

We report here the solid-phase synthesis of Mappicine ketone library, as an antiviral lead compound with selective activity against herpes viruses (HSV-1 and HSV-2) and human cytomegaloviruses, based on three chemoselective palladium(0)-catalyzed reactions involving intramolecular Heck reaction at C-2, functionalization including Suzuki-Miyaura cross-coupling reaction, amination and thioetherification at C-7 and cleavage of benzenesulfonate linker at C-10. We have developed the palladium-catalyzed reductive cleavage of the sulfonate linker to release the parent arene including electron-donating groups, which was difficult so far. Furthermore, cleavage of the sulfonate linker with functionalization could also be achieved by the palladium- or nickel-catalyzed reaction.

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