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. 2017 Jun 29;32(1):850–864. doi: 10.1080/14756366.2017.1334648

Scheme 1.

Scheme 1.

Reagents and conditions: (a) i) ArCO2H, SOCl2, DMF, DCM, ii) Et3N, EtOAc, aminophenol (1a–d); iii) NaOH, EtOH/H2O, then 6 M HCl, 60–80% over 2 steps; (b) APTS, toluene, reflux, 70–80%, (c) T3P® (50% in EtOAc), DIPEA, 3,4-dimethoxybenzoic acid, 35%.