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. 2020 Oct 7;63(20):11615–11638. doi: 10.1021/acs.jmedchem.0c00793

Scheme 5. Syntheses of AR Ligand-Based PROTACs 2127.

Scheme 5

Reagents and conditions: (a) tert-butyl bromoacetate, K2CO3, ACN, rt; (b) 4.0N HCl in dioxane, rt; (c) HATU, DIPEA, dry DMF, rt; (d) PPh3, DIAD, dry THF, 0 °C-rt; (e) DIPEA, dry DMF, 70 °C.