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. 2014 Dec 4;6(3):276–281. doi: 10.1021/ml500420y

Scheme 1. Synthesis of Sulfonamides 3, 4, and 9–33.

Scheme 1

Reagents and conditions: (a) Pd(OAc)2, RuPhos, NaOt-Bu, 1,4-dioxane, 100 °C; (b) HCl, H2O, THF, 23 °C, 60% (2 steps); (c) cyclobutylamine, NaBH(OAc)3, AcOH, 1,2-DCE, 23 °C, quant.; (d) R-SO2Cl, DIPEA, CH2Cl2, 23 °C, 29–57%.