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Reagents and conditions, a) s-BuLi, TMEDA, Et2O, −78 °C, 30 min, then Mel, −78 °C to 25 °C, 8 h, 86%; b) TFA:CH2Cl2 (3:1), 25 °C, 1 h; c) 23, EDCI, HOBt, DIPEA, CH2Cl2, 0 °C to 25 °C, 12 h, 66% (2 steps); d) LiOH·H2O, THF:H2O (2:1), 25 °C, 6 h, 88%; e) 18b, EDCI, HOBt, DIPEA, CH2Cl2, 0 °C to 25 °C, 12 h, 48%.
