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. Author manuscript; available in PMC: 2012 Dec 13.
Published in final edited form as: J Med Chem. 2011 Oct 3;54(20):7375–7384. doi: 10.1021/jm2009937

Scheme 1. Scaffold Synthesis.

Scheme 1

Reagents and conditions: (a) Boc-Gly-OH, HCTU, DIEA, DMF, rt, 92 %; (b) LiOH (2N), THF, rt, 95 %; (c) β-Ala-OMe, BOP, DMF, DIEA, rt, 85 %; (d) LiOH (2N), THF:MeOH, 0°C, 90 %; (e) PtO2, H2, 50 psi, MeOH:CHCl3, rt, 80%; (f) Boc2O, DIEA, H2O:MeCN, rt, 80%; (g) Fmoc-OSu, H2O:MeCN, NaHCO3 0°C to rt, 65 %.