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. Author manuscript; available in PMC: 2020 May 27.
Published in final edited form as: J Med Chem. 2019 May 9;62(10):5217–5241. doi: 10.1021/acs.jmedchem.9b00532

Scheme 1. Synthesis of aromatic and heteroaromatic sulfonamide analogs via sulphonylation / cross-couplinga.

Scheme 1.

aReagents and conditions: (a) amine 1a-d, 1f-j, RSO2Cl, iPr2NEt, CH2Cl2, rt; (b) amine 1e, 1k-m, RSO2Cl, K2CO3, CHCl3/H2O (1/1), rt; (c) Pd/C, H2, MeOH, rt; (d) ArB(OH)2, Pd(PPh3)4 (10 mol%), aq. Na2CO3 (2 M)/THF (1/10), reflux. Mes, mesitylene, 2,4,6-Me3Ph.