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. 2015 Mar 22;6(5):537–542. doi: 10.1021/acsmedchemlett.5b00026

Scheme 2. Synthesis of 1,3-Dihydroxypyridin-4-one Derivatives.

Scheme 2

(a) 6a: m-CPBA, TFA, DCM, 69%. Or 6b: 50% H2O2, AcOH/THF 1:1, 60 °C, 34%. (b) (i) MSTFA, THF; (ii) CSI, DCM, 0 °C; (iii) THF, 0 °C to rt, 24% 8a, 48% 8b; (c) Pd black, H2, EtOH, 58% 8a, 46% 8b; (d) TFA, DCM 0 °C, 54% 9a, 38% 9b.