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. 2013 Mar 21;56(7):2975–2990. doi: 10.1021/jm400009c

Scheme 1. General Synthetic Approach to Pyrrolones.

Scheme 1

(a) Chloroacetyl chloride, pyridine, 0 °C, 30 min, 75%; (b) KOH, EtOH, 95%; (c) p-toluenesulfonic acid bound with silica gel, 15–20 min, microwave, 80–90%, or p-toluenesulfonic acid, toluene, 90 °C, 3 h Dean–Stark apparatus; (d) POCl3, DMF, 100 °C, 3 h, 80–95% ; (e) KHSO4, EtOH, 3 h, reflux, 80–95%; R and R1 as defined in Tables 1 and 3.