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(a) 1. SOCl2, 90 °C, 2 h, 2. (R)-1-Boc-piperazine-2-carboxylic acid, DCM/pyridine/DMF, r.t., 20 h; (b) Benzyl bromide, KHCO3, 65 °C, 18 h; (c) HCl, DCM, r.t., o.n.; (d) 1. D-(-)-3-Acetylthio-2-methylpropionic acid, SOCl2, DCM/DMF, 0 °C–rt, o.n., 2. DIPEA, DCM, r.t., 18.5 h; (e) LiOH, H2O/THF, r.t., 4 h; and (f) BBr3, DCM, −78 °C–r.t., o.n.
