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a) p-toluenesulfonic acid monohydrate, CH2Cl2, r.t., 24h; b) i -oxalyl chloride, dry CH2Cl2, r.t., 15h; ii - cold 25% ammonium aq. solution, dry THF, 2h; c) RNH2, dry THF, Et3N, T3P(50 wt. % in THF), ice; d) T3P (50 wt. % in THF), THF/EtOAc, Et3N, 77°C , 5h.
