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. 2017 Jul 10;8(8):886–891. doi: 10.1021/acsmedchemlett.7b00230

Scheme 2. Representative Synthesis of 2-Thiohydantoin Derivative 76.

Scheme 2

Reagents and conditions: (a) THF, 4 °C–rt, yield 62%; (b) paraformaldehyde, AcOH, NaCNBH3, yield 94%; (c) Pd/C, H2, MeOH, yield 60%; (d) CSCl2, DCM-aq·NaHCO3, 4 °C–rt, yield 94%; (e) EtOH, rt, yield 84%.