Scheme 2.
Synthesis of VHL-based compounds 21a and 21b. Reagents and conditions: (a) N,N-diisopropylethylamine, HATU, DMF, rt, 12 h, 35–55%; (b) TFA, DCM, rt, 0.5 h; (c) 9, DMAP, pyridine, rt, 16 h, 45%–65%; (d) BF3·OEt2, MeCN, 0 °C, 0.5 h, 55%–60%.
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