反应详情

A mixture of 2-guanidinoindole-3-carboxylic acid ethyl ester hydrochloride (1.00 g, 3.5 mmol) and sodium hydroxide (1.5 g) in water (50 mL) is heated to gentle reflux for 6 hr followed by the addition of sufficient 5% HCl to adjust the solution to pH 1, and filtration of the resulting mixture through celite, washing the pad with water. The filtrate is extracted with ethyl acetate (3×25 mL), and then basified with solid sodium carbonate. The tan precipitate which slowly forms is collected by filtration, washed with water, and dried in vacuo affording 2-amino-4-oxo-3H-indolo[2,3-d]pyrimidine (561 mg, 78%) as light tan crystals, mp >275 C.

1. temperatureis heated
2. temperatureto gentle reflux for 6 hr
3. filtrationto pH 1, and filtration of the resulting mixture through celite
4. washwashing the pad with water
5. extractionThe filtrate is extracted with ethyl acetate (3×25 mL)
6. filtrationThe tan precipitate which slowly forms is collected by filtration
7. washwashed with water
8. customdried in vacuo