General Procedure H. Azide (1.0 eq.) was dissolved in MeOH (58 mL/mmol). A catalytic amount of 10 wt.% Pd/C was added, and the reaction was stirred under an atmosphere of H2 for 16 h. The reaction mixture was then filtered through PTFE syringe filters and evaporated to dryness to obtain the desired amine quantitative yields. The resulting amine (1.0 eq.) was added to a solution of thalidomide derivatives 19, 65 or 87 (1.0 eq.) and DIPEA (4.0 eq.) in DMSO (24 mL/mmol) and the reaction was left to stir in a sealed vial at 90°C for 4 h. the reaction was then purified by HPLC using a linear gradient of 5% to 95% MeCN in 0.1% HCOOH in water over 10 min gradient unless otherwise stated. Azide 20 was dissolved in MeOH (600 µL). A catalytic amount of 10 wt.% Pd/C (3 mg) was added, and the reaction was stirred under an atmosphere of hydrogen for 24 h. The reaction mixture was then filtered through a PTFE syringe filter and evaporated to dryness to leave crude amine intermediate. The crude amine (8 mg, 7.2 µmol) was dissolved in DMF (100 µL) and added to a solution of (+)-JQ1-acid (3 mg, 7.5 µmol), HATU (3 mg, 7.9 µmol) and DIPEA in DMF (400 µL) and stirred at r. Azide 21 was dissolved in MeOH (600 µL). A catalytic amount of 10 wt.% Pd/C (3 mg) was added, and the reaction was stirred under an atmosphere of hydrogen for 24 h. The reaction mixture was then filtered through a PTFE syringe filter and evaporated to dryness to leave crude amine intermediate. The crude amine was dissolved in DMF (100 µL) and added to a solution of (+)-JQ1-acid (5 mg, 12.4 µmol), HATU and DIPEA 1403.5402.