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. 2020 Apr 3;11(6):1269–1273. doi: 10.1021/acsmedchemlett.0c00111

Scheme 1. Synthesis of Compounds TMX-1120, TMX-2164, and TMX-2177.

Scheme 1

Reagents and conditions: (a) 5, TEA, DMSO, 95 °C, 67%; (b) DABSO, PdCl2(AmPhos)2, TEA, i-PrOH, 75 °C; then NFSI, rt, 6% (for TMX-1120) or 7% (for TMX-2164); (c) 5 or 8, TEA, DMF, MeOH, 70 °C, 59% (for 9) or 9% (for TMX-2177).