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. Author manuscript; available in PMC: 2017 Apr 28.
Published in final edited form as: J Med Chem. 2016 Apr 6;59(8):3635–3649. doi: 10.1021/acs.jmedchem.5b01718

Scheme 1.

Scheme 1

Synthesis of linker region intermediate.a

aReagents and conditions: (a) K2CO3, reflux, 12 h, 82%; (b) Pd/C, NH2NH2•H2O (10 eq), reflux, 3.5 h, 71%; (c) Pyr (17 eq), ClCOOPh (1.1 eq), 3 h, 90%; (d) NH2NH2•H2O (5.5 eq), reflux, 3 h, quant; (e) formamidine acetate (4.5 eq), acetic acid, reflux, 3 h, 91%.