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. Author manuscript; available in PMC: 2016 Nov 15.
Published in final edited form as: J Med Chem. 2015 Nov 9;58(22):8970–8984. doi: 10.1021/acs.jmedchem.5b01321

Scheme 1. Synthesis of Bis-arylamide Inhibitors of STAT6a.

Scheme 1

aReagents and conditions: (a) EDC, 4-iodoaniline (for 34a) or aniline (for 34b), DCM, rt 12 h; (b) Ph3Bi, Cu(OAc)2, TEA, DCM, 24 h; (c) (i) neat TFA, (ii) Boc-Tle-OH, HBTU, DIPEA, DCM rt 6 h; (d) neat TFA; (e) NMP, NMM, DMAP (cat), rt, 3 h; (f) (i) HBTU, DIPEA, DCM, 6 h, (ii) neat TFA, 1 h.