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. Author manuscript; available in PMC: 2024 Mar 5.
Published in final edited form as: Eur J Med Chem. 2022 Dec 30;249:115043. doi: 10.1016/j.ejmech.2022.115043

Scheme 4. Preparation of aryl chlorides 118, 119, 122, 124, 127a.

Scheme 4.

aReagents and conditions: (a) BBr3, DCM, 0°C-rt, 18 h, 42%; (b) diiodomethane or 1,2-dibromoethane, K2CO3, DMF, 60°C, 2 h, 53–66%; (c) (i) DMF-DMA, DMF, 150°C, 3 h, (ii) MeCN, nBuLi, THF, −78°C, 1 h, 80% (over two steps); (d) POCl3, neat, 100°C, 2 h, 50–95%; (e) POCl3, THF, 66°C, 1 h, 86%; (f) formamide, neat, 160°C, 24 h, 52%.