1: 1.) LDA, I2, 2.) DBU / 1.) THF, -78 deg C, 1.5 h, 2.) 0 deg C, 1 h, room temperature, 48 h 2: 2.) 2,6-di-tert-butylphenol / 1.) toluene, -78 deg C, 2.) THF, -78 deg C to room temperature, 30 min 3: 75 percent / 1.) H2, 2.) HCl / 1.) Pd-C / 1.) AcOH, 50 deg C, 4 bar, 2.) MeOH 4: 95 percent / TFA / 16 h / Ambient temperature View Scheme