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. 2021 Nov 29;64(23):17031–17050. doi: 10.1021/acs.jmedchem.1c00605

Scheme 1. Synthesis of Compounds 213.

Scheme 1

Reagents and conditions: (a) methyl iodide, dry DMF, rt; (b) (cyclo)alkyl-/arylalkyl bromide, anhydrous potassium carbonate, dry DMF, rt; (c) (i) cesium carbonate, MeOH, rt, (ii) methyl iodide, dry DMF, 0 °C → rt; (d) ethyl propiolate, tetrabutylammonium fluoride, dry THF, rt; and (e) potassium hydroxide 2 N, ethanol, rt.