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. Author manuscript; available in PMC: 2013 Apr 12.
Published in final edited form as: J Med Chem. 2012 Mar 20;55(7):3088–3100. doi: 10.1021/jm2015183

Scheme 5.

Scheme 5

Preparation of Compounds with Modified Linkers

Reagents and conditions: (a) pyridine, reflux, 4 h; (b) 200 °C, 1 h; (c) NH2OH·HCl, NaOAc, absolute EtOH, 16 h; (d) pyridine, CH2Cl2, ethyl 3-chloro-3-oxopropanoate, room temp, 18 h; (e) THF, LiOH, room temp, overnight; (f) DIPEA, BOP-Cl, 4-ethylaniline, room temp, 22 h; (g) Pd(OH)2/C (25 wt %), EtOH-cyclohexene (2:1), reflux, 2.5 h.