First asymmetric synthesis of CJ-14877 and its enantiomer and their interleukin-1β inhibitory activities

Bioorganic & Medicinal Chemistry Letters
2009.0

Abstract

A potent antiinflammatory methyl picolinate alkaloid CJ-14877 [(+)-1] and its enantiomer (-)-1 were synthesized in two steps starting from commercially available methyl 5-bromopicolinate. The synthesis includes microwave-assisted Suzuki coupling reaction and Sharpless asymmetric dihydroxylation.

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