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Reagents and conditions: (a) TEA, Boc2O, 1,4-dioxane, H2O, room temperature, 24 h; (b) MeOH, SOCl2, reflux, 3 h; (c) DIPEA, HATU, DMF, 50 °C, 24 h; (d) (1) 1 M NaOH, MeOH, reflux, 2 h; (2) TFA, DCM, room temperature, 2 h; (e) DIPEA, HATU, NH2OTHP, DMF, 50 °C, 24 h; (f) (1) E3 ligase ligand-linker-COOH 43a,b/HyT-linker-COOH 47a,b (see Scheme S4.1 in Supplementary Materials.), DIPEA, HATU, DMF, 50 °C, 24 h; (2) 1 M HCl, THF, US, room temperature, 2 h.
