Dicyclohexylcarbodiimide → Camptothecin

Participants

Reaction Steps

The synthesis is shown in FIG. 6. 1 g of Y-shape branched PEG carboxylic acid (Example 5 or 6) was dissolved in 10 ml dichloromethane. 120 mg of glycine-camptothecin, 50 mg of dimethylamino pyridine and 95 mg of dicyclohexylcarbodiimide were added to the solution. The solution was stirred at room temperature for 6 hours. The solvent was removed under vacuum. The residue was dissolved in 20 ml of 1,4-dioxane. The precipitate was removed by filtration. The solution was concentrated, and the residue was added to 20 ml of ethyl ether. The precipitate was collected by filtration, washed with ethyl ether and dried under vacuum. Yield: 0.8 g (80%), Mp: 56-58° C.

Provenance & Evidence