Scheme 15
From: Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs
Chemical synthesis of other cereblon-binding scaffolds based PROTACs. Reagents and conditions: a PdCl2(dppf)×CH2Cl2, K3PO4, dioxane/H2O, 100 °C, 16 h; b K2CO3, DMF, rt, 3 h; c Pd/C, H2, EtOH, RT, 16 h; d TFA, CH2Cl2, rt, 2 h; e1 10% Pd/C, triethylsilane, EtOH, 90 min; e2 H2 (15 psi), 10% Pd/C, THF, rt, 4 h; f (i) (COCl2), DMF (cat.), CH2Cl2, 0 °C, 2 h; (ii) ArCOCl, Et3N, CH2Cl2, 0 °C to rt, 18 h; g THF, 75 °C, 1 h.
