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. 2016 Jan 15;26(2):355–360. doi: 10.1016/j.bmcl.2015.12.003

Scheme 2.

Scheme 2

Reagents and conditions: (i) 2-bromothiophene, DMSO, KF, PdCl2(PPh3)2, AgNO3, 100 °C, N2, 2 h; (ii) (a) THF, pyridine, pentafluorophenyltrifluoroacetate, rt, 2 h; (b) THF, methylamine (40% soln.) or dimethylamine, rt, 2–3 h; (iii) toluene/EtOH, 2 M Na2CO3, PdCl2(dppf)·CH2Cl2, 85–90 °C, N2, 2–6 h.