Extended Data Fig. 6 | Nature Cancer

Extended Data Fig. 6

From: Targeting a lineage-specific PI3Kɣ–Akt signaling module in acute myeloid leukemia using a heterobifunctional degrader molecule

Extended Data Fig. 6

Synthetic scheme for the synthesis of the PIK3CG degrader, ARM165. Reagents and conditions: i) LiOH monohydrate, MeOH, H2O, 60 °C, 40 h (94%); ii) Boc-AOc-OH, T3P 50% in ethyl acetate, pyridine, N,N-dimethylformamide, 80 °C, 16 h; iii) TFA, CH2Cl2, r.t. 2 h; iv) Glutaric anhydride, N,N-diisopropylethylamine, toluene, N,N-dimethylformamide, 110 °C, 2 h (62% over 3 steps, ii-iv); v) Compound I, HATU, N,N-diisopropylethylamine, N,N-dimethylformamide, r.t. 16 h (55%).

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