| 摘要 |
Preparation of 2-fluoroadenine, comprises: converting 2,6-diaminopurine in a water-free fluorinating agent in the presence of a nitrite; heating the reaction mixture after adding the nitrite; mixing and quenching the heated reaction mixture under stirring in water; separating, preferably filtering the obtained mixture; washing the solid materials with water; and separating, preferably filtering the obtained solid material without additional cleaning steps and drying to obtain the 2-fluoroadenine (53-68, preferably 54-60%) with a purity of at least 98%. Preparation of 2-fluoroadenine, comprises: converting 2,6-diaminopurine in a water-free fluorinating agent in the presence of a nitrite at -30 to -10[deg] C, preferably -20 to -12[deg] C; heating the reaction mixture after adding the nitrite for a period of 0.5-4 hours, preferably 1-1.5 hours at -5 to 5, preferably 0[deg] C; mixing and quenching the heated reaction mixture under stirring in 7-13 folds, preferably 8 folds of water quantity in kilogram, relative to the used quantity at fluorinating agent in kilogram; separating, preferably filtering the obtained mixture; washing 4-7, preferably 5 folds of solid materials with 7-13, preferably 8 folds of water quantity, which is in kilograms, relative to the fixed quantity of fluorinating agents in kilograms; and separating, preferably filtering the obtained solid material without additional subsequent cleaning steps and drying at 70-85, preferably 80[deg] C in the vacuum to obtain 2-fluoroadenine (53-68, preferably 54-60%) with a purity of at least 98%. |
