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. Author manuscript; available in PMC: 2011 May 13.
Published in final edited form as: J Med Chem. 2010 May 13;53(9):3632–3644. doi: 10.1021/jm1000612

Scheme 3a.

Scheme 3a

a Reagents and conditions: (a) Lawesson’s reagent (1 equiv for 9a, excess for 9b), toluene, 80 °C; (b) HF-pyridine, rt; (c) DAST, CH2Cl2, −78 °C; (d) BrCCl3, DBU, CH2Cl2, 0 °C to rt; (e) LiOH, THF/H2O, Δ; (f) (2 mM in DMF), EDC, HOBT, 2,6-lutidine, 1,3-bis(aminomethyl)benzene rt, 2 d.