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. Author manuscript; available in PMC: 2017 Dec 22.
Published in final edited form as: J Med Chem. 2016 Dec 2;59(24):11148–11160. doi: 10.1021/acs.jmedchem.6b01450

Scheme 1.

Scheme 1

Synthetic route to 1a

a Reagents and conditions: (a) thiourea, n-BuOH, reflux, 3 h, quantitative; (b) bromoacetyl bromide, DMAP, DCM, 0 °C to rt, 12 h, 88%; (c) NaOEt, EtOH, reflux, 1 h, 58%.