تفاعل #85935

معادلة التفاعل

dioxane

3-chloro-2-(4-(6-fluoropyridin-2-yl)benzyl)-7-isobutyl-5-methyl-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione

potassium carbonate

phenol

→

pure product

المردود 67.4%

2-(4-(6-fluoropyridin-2-yl)benzyl)-7-isobutyl-5-methyl-3-phenoxy-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione

المردود 67.4%

المذيبات

DMF

ظروف التفاعل

المعالجة

1. 1
   أخرىThe vial is sealed
2. 2
   ترشيحfiltered
3. 3
   أخرىThe filtrate is purified with a semi-preparative HPLC

الإجراء التجريبي

3-chloro-2-(4-(6-fluoropyridin-2-yl)benzyl)-7-isobutyl-5-methyl-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione (40 mg, 0.095 mmol), potassium carbonate (40 mg, 0.28 mmol) and phenol (26 mg, 0.28 mmol) are placed in a Biotage microwave vial, and then 0.4 mL of dioxane is added. The vial is sealed, and then heated in a Biotage microwave instrument at 150° C. for 3 h. The reaction mixture is diluted with DMF, and then filtered. The filtrate is purified with a semi-preparative HPLC to give 32 mg of pure product as pale yellow crystals (Purity: 99.9%). MS (ESI) m/z 500.2 [M+H]+.

المصدر