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. 2022 Apr 19;13(5):841–847. doi: 10.1021/acsmedchemlett.2c00100

Scheme 1. Synthesis of MrgX1 PAMs.

Scheme 1

Reagents and conditions: (a) NaHCO3, H2O, rt, 12 h; 25–80% (b) T3P, Et3N, CH2Cl2, rt, 6 h; 65% (c) HATU, iPr2NEt, THF, rt, 16 h; (d) AcOH, 80 °C, 16 h; 93% 2 steps (e) K2CO3, BuOH, 150 °C; (f) Et3N, CH2Cl2; 7% 2 steps (g) POCl3, 25%.