Реакция #8682

Уравнение реакции

water

sodium carbonate

3-[5-(2,5-diazabicyclo[2.2.1]hept-2-yl)-2-pyrimidinyl]-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine

2-iodopropane

→

1-(2-Fluorobenzyl)-3-[5-(5-isopropyl-2,5-diazabicyclo[2.2.1]hept-2-yl)-2-pyrimidinyl]-1H-pyrazol[3,4-b]pyridine

Растворители

acetone

Условия реакции

Обработка

1. 1
   Экстракцияextracted with DCM
2. 2
   Промывкаwashed with saturated aqueous sodium chloride solution
3. 3
   Другоеdried
4. 4
   Фильтрацияfiltered
5. 5
   ДругоеThe solvent is removed in vacuo
6. 6
   Другоеthe residue is purified by preparative HPLC with addition of small portions of aqueous hydrochloric acid
7. 7
   Другое25 mg (42% of theory) of the product are obtained

Методика

50 mg (0.13 mmol) of 3-[5-(2,5-diazabicyclo[2.2.1]hept-2-yl)-2-pyrimidinyl]-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine (example 9) are dissolved in 5 ml of absolute acetone, and 92 mg (0.87 mmol) of sodium carbonate are added. 64 mg (0.37 mmol) of 2-iodopropane are added to the suspension, and the mixture is stirred at RT overnight. The reaction solution is mixed with water and extracted with DCM. The organic phases are combined, washed with saturated aqueous sodium chloride solution, dried and filtered. The solvent is removed in vacuo, and the residue is purified by preparative HPLC with addition of small portions of aqueous hydrochloric acid. 25 mg (42% of theory) of the product are obtained.

Источник