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. 2022 Jul 7;23(14):7535. doi: 10.3390/ijms23147535

Scheme 3.

Scheme 3

Reagents and conditions: (a) DMF, C5H5N, C2O2Cl2, room temperature, 6 h; (b) (1) C5H5N, room temperature, 24 h; (2) 1 M NaOH, MeOH, reflux, 2 h; (c) (1) DIPEA, HATU, NH2OBn·HCl, DMF, 50 °C, 24 h; (2) TFA, DCM, room temperature, 2 h; (d) (1) E3 ligase ligand-linker-COOH 43b/HyT-linker-COOH 47b (see Scheme S4.1 in Supplementary Materials), DIPEA, HATU, DMF, 50 °C, 24 h; (2) Pd/C (5%), H2, THF, 24 h.