Scheme 7
From: Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs
Chemical synthesis of 5-Aminothalidomide based PROTACs. Reagents and conditions: a 3-aminopiperidine-2,6-dionehydrochloride, potassium acetate, acetic acid, 90 °C, overnight; b DIPEA, N-methyl-2-pyrrolidone (NMP), 90 °C, overnight (depending on the type of linker); c Propargylamine, DIPEA, DMF, 90 °C, 12 h; d Copper (II) sulfate × 5 H2O, sodium ascorbate, H2O/tert-butanol, rt, 16 h (depending on the type of linker).
