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. Author manuscript; available in PMC: 2014 Apr 11.
Published in final edited form as: J Med Chem. 2013 Mar 25;56(7):2747–2763. doi: 10.1021/jm301253y

Scheme 1.

Scheme 1

Reagents and conditions: a) 20% Piperidine/DMF; b) 3 eq Fmoc-Xaa-OH, 3 eq BOP or HBTU, 6 eq DIEA, DMF; c) Fmoc-Yaa-aldehyde, NaBH3CN, AcOH, DMF; d) Fmoc-Cys(SBut)-OH, BOP or HBTU, DIEA, DMF; e) (ClCH2CO)2O, NEM, DCM; f) Bu3P/H2O/THF; g) NEM, DMF, heat 5560°C; h) TFA/TIS/EDT/H2O 91:3:3:3