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. 2014 Nov 10;57(23):10176–10191. doi: 10.1021/jm501578n

Scheme 3. Preparation of Compound 9.

Scheme 3

Reagents and conditions: (a) isopropylamine, triethylamine, THF, rt, 3 h, quant.; (b) 22, Pd2dba3, X-Phos, Cs2CO3, 1,4-dioxane, reflux, 3 h, 72%; (c) Pd/C, EtOAc, MeOH, H2, rt, 18 h, 92%; (d) trimethyl orthoformate, formic acid, 100 °C, 1 h, 27%.