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. 2021 Sep 28;6(40):26583–26600. doi: 10.1021/acsomega.1c03948

Scheme 5. Synthesis of Colchicine Derivatives (8 and 29–43).

Scheme 5

Reagents and conditions: (a) propargylamine or respective amide/carbamate of propargylamine, CuSO4, sodium ascorbate, MeOH/H2O 10/1 v/v, 55 °C for 8, 29–40, and 43; (b) di-tert-butyl dicarbonate, Et3N, DCM, RT for 41; (c) 2,2,2-trichloroethyl chloroformate, Py, DCM, 0 °C to RT for 42.