反应详情

To a stirred solution of 5-benzyloxy-6-hydroxy-2-(1-pyridin-2-yl-cyclopentylmethyl)-pyrimidine-4-carboxylicacidcyclopropyl-(2-hydroxyethyl)-amide (451) (80 mg, 0.164 mmol), in dichloromethane (6 mL), TPP (150.33 mg, 0.574 mmol) and diisopropyl azodicarboxylate (0.097 mL, 0.492 mmol) were added and stirring was continued for 1 h at room temperature while silica thin layer chromatography was performed (100% ethyl acetate, Rf=0.2). After completion of the reaction, water (5 mL) was added and the mixture was extracted with dichloromethane (2×25 mL). The combined extracts were dried and concentrated to get crude 9-benzyloxy-2-cyclopropyl-6-(1-pyridin-2-yl-cyclopentylmethyl)-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,8-dione (452) (270 mg, Crude) as a yellow gummy liquid.

1. additionwas added
2. extractionthe mixture was extracted with dichloromethane (2×25 mL)
3. customThe combined extracts were dried
4. concentrationconcentrated