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. 2021 Apr 4;82(7):883–895. doi: 10.1002/ddr.21814

SCHEME 3.

SCHEME 3

Synthesis of key intermediate 15 (route 2). aReagents and Conditions. a. FeCl3/AlCl3, 0 to −10 °C (Yield: 81%); b. isoquinoline/pTSA 180–220 °C; c. i) EtOH, PTC, KOAc, toluene; ii) trichloroisocyanuric acid, 0–5 °C; iii) NaHCO3; (Yield: 75%); d. PPh3, MeOH (Yield: 99%); e. 0–5 °C, 35% H2O2; f. H+ (Yield: 80%)