SYNTHESIS OF A NEW OSELTAMIVIR DERIVATIVE THROUGH LATE-STAGE CATALYTIC C-H FUNCTIONALIZATION

[摘要]：N-Boc-protected oseltamivir 5 was converted to olefin insertion product 4 via a ruthenium-catalyzed C(sp(2))-H functionalization reaction using its ester functionality as a directing group. The addition of a catalytic amount of (p-CF3C6H4)(3)P in the presence of the RuH2(CO)(PPh3)(3) catalyst significantly improved the yield for this specific conversion. Tamao-Fleming oxidation followed by deprotection concisely produced a new oseltamivir analog 16.

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