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Reagents and conditions: (a) (1) K2CO3, DMF, room temperature, 1 h; (2) propargyl bromide at 0 °C; (3) 24 h at room temperature; (b) (1) toluene, reflux, 2 h; (2) THF, 0 °C, CH₃COOH, Na(CH₃COO)₃BH, 30 min; (3) 24 h, room temperature; (c) DIPEA, HATU, NH2OTHP, DMF, 50 °C, 24 h; (d) (1) E3 ligase ligand-linker-N3 50 (see Scheme S4.2 in Supplementary Materials), THF/H2O, Sod. Ascorbate, CuSO4 × 5H2O, 24 h, room temperature; (2) 1 M HCl, THF, US, room temperature, 2 h.
