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. Author manuscript; available in PMC: 2013 Apr 26.
Published in final edited form as: J Med Chem. 2012 Apr 18;55(8):3725–3738. doi: 10.1021/jm201544y

Scheme 1a.

Scheme 1a

aConditions: (a) 1,4-dioxane-2, 6-dione, DMF, r.t., (87–92%); (b) tert-butyl-12-amino-4,7,10-trioxadodecanoate, DIEA, HOBt, EDCI, DMF, 72 h, r.t., (77–82%); (c) TFA, dichloromethane, 4 h, (88.3–89.3 %); (d) DIEA, HOBt, TBTU, EGFR-L1 or EGFR-L2, DMF, 24 h, then TFA/H2O/phenol/TIS 88/5/5/2 (20–80%).