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. 2021 Apr 14;64(9):6241–6261. doi: 10.1021/acs.jmedchem.1c00263

Scheme 4. Synthesis of Aminothiophene Intermediates 16a, 16b, and 19.

Scheme 4

Reagents and conditions: (a) phosphorus oxychloride, DMF, toluene, 80 °C, 3 h; (b) 2,5-dihydroxy-1,4-dithiane, Et3N, CH3OH, 50 °C, 2.5 h; (c) oxalyl chloride, 1,2-dichloroethane, reflux, 4 h; (d) ethylamine, CH3CN, −10 °C, 3 h.