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. Author manuscript; available in PMC: 2017 Mar 24.
Published in final edited form as: J Med Chem. 2016 Mar 15;59(6):2579–2595. doi: 10.1021/acs.jmedchem.5b01780

Scheme 3a.

Scheme 3a

aReagents and conditions: (i) AlCl3, CH2Cl2, r.t., overnight; (ii) methyl acrylate, Pd(OAc)2, NEt3, DMF, 100°C, 6 h; (iii) LiOH aq. 1N, THF, reflux, 3 h or r.t., overnight; (iv) H2, Pd/C, EtOH/EtOAc 20 psi, 7–12 h; (v) (CH2OH)2, pTsOH, toluene, reflux, overnight; (vi) (CH2SH)2, BF3.Et2O, CH2Cl2, r.t., 0.5–1 h; (vii) I2, acetone, 4Å MS, reflux, 16 h.