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Synthetic route of PROTACs. (A) Synthesis of S3I-201 analogs. (B) Synthetic of PROTACs. Reagents and conditions: (a) THF, 0°C, 3 h; (b) 5% NaOH aq, EtOH, rt, 3 h; (c) SOCl2, 80°C, reflux, 2 h; (d) THF, Et3N, 0°C, overnight, rt; (e) 3-Aminopiperidine-2,6-dione hydrochloride, CH3COONa, CH3COOH, 100°C, 16 h; (f) BocNH-Linker-NH2, DIPEA, DMF, 80°C; (g) DCM, CF3COOH, rt, 2 h; (H) HATU, DIPEA, DCM, rt, 12 h.
