Skip to main content
. Author manuscript; available in PMC: 2022 Feb 25.
Published in final edited form as: J Med Chem. 2020 Nov 17;63(23):14951–14978. doi: 10.1021/acs.jmedchem.0c01464

Scheme 3. Functionalization of the Lactam Nitrogen.

Scheme 3.

(a) copper iodide (CuI, 20 mol%), N,N’-dimethylethylenediamine (40 mol%), cesium carbonate (Cs2CO3), ArI, toluene, 80 °C, 20 h; (b) sodium hydride (NaH, 60% dispersion), para-toluenesulfonyl chloride (p-TsCl), DMF, 0 °C 2 h; (c) di-tert-butyl dicarbonate (boc2O), N,N-dimethylaminopyridine (DMAP), Et3N, CH2Cl2, 0 °C to rt, 2 h.