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. 2021 Apr 27;64(9):5905–5930. doi: 10.1021/acs.jmedchem.1c00047

Scheme 12. Synthesis of Compounds 39, 40, and 44–46.

Scheme 12

Reagents and conditions: (a) DIPEA, 1,4-dioxane, 120 °C, 18 h, 56%; (b) POCl3, 80 °C, 1 h, 67%; (c) (i) Pd/C, H2, MeOH, RT, 18 h; (ii) CDI, DIPEA, DCM, 18 h, then pyrrolidine, RT, 4.5 h, 22–46%.