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. 2022 Feb 10;13(3):377–387. doi: 10.1021/acsmedchemlett.1c00448

Scheme 6. Synthesis of Compounds 15.

Scheme 6

Reagents and conditions: (a) Pd(dba)2, xantphos, Cs2CO3, dioxane, 110°C, 2 h, 89%; (b) HCl/EtOAC, 15°C, 2 h; (c) tetrahydropyran-4-one, tetramethylammonium, triacetoxyboranuide, TFA, DCM, 15°C, 2 h; (d) acetaldehyde, tetramethylammonium, triacetoxyboranuide, TFA, DCM, 15°C, 2 h; (e) TFA, DCM, 45°C, 2 h, 14% (3 steps).