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

Scheme 4. Synthesis of Colchicine Derivatives (9 and 2428).

Scheme 4

Reagents and conditions: (a) propargyl alcohol or respective ester of propargyl alcohol, CuSO4, sodium ascorbate, MeOH/H2O 10/1 v/v, 55 °C for 9, 26, and 27; (b) respective carboxylic acid, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDCI), 4-(dimethylamino)pyridine (DMAP), DCM, RT for 24, 25, and 28.