Skip to main content
. 2020 May 24;25(10):2448. doi: 10.3390/molecules25102448

Scheme 9.

Scheme 9

Synthesis of apalutamide via late-stage, thiophosgene-free cyclization. Reaction conditions: (a) 12, CDI, DBU, i-Pr2NEt, THF, 60 °C; (b) HCl, 2-PrOH, 70 °C; (c) 28, DMA, KOAc, CuBr, TMEDA, 120 °C; (d) 1,1′-thiocarbonylbis(pyridine2(1H)-one, DMAP, DMA, 90 °C.