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Reagents and conditions: (i) tosyl chloride (TsCl), DCM, 4-dimethylaminopyridine (DMAP), TEA, 0 °C; (ii) HNR1R2, MeCN, K2CO3, reflux; (iii) Cs2CO3, tris(dibenzylideneacetone)dipalladium (Pd2(dba)3), Xantphos, dioxane, reflux; (iv) MeOH, Pd/C, H2, rt; (v) MeOH, reflux.
