反应详情

温度

90 °C

tert-Butyl [1-(aminocarbonothioyl)piperidin-4-yl]carbamate (Intermediate 125, 400 mg) was dissolved in anhydrous EtOH (5 ml). Ethyl 2-chloro-4-(2-methoxyethoxy)-3-oxobutanoate (Intermediate 124, 368 mg) was added and the mixture was heated at 90° C. for 18 h. Partial removal of Boc group was detected. Solvent was removed in vacuo and the dried material was treated with 4 N HCl/dioxane for 2 h. Solvent was removed in vacuo to give a brown/yellow solid which was dried to afford the title compound which was used without further purification (508 mg).

1. customPartial removal of Boc group
2. customSolvent was removed in vacuo
3. additionthe dried material was treated with 4 N HCl/dioxane for 2 h
4. customSolvent was removed in vacuo
5. customto give a brown/yellow solid which
6. customwas dried