تفاعل #8682

معادلة التفاعل

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

المذيبات

acetone

ظروف التفاعل

المعالجة

1. 1
   استخلاصextracted with DCM
2. 2
   غسيلwashed with saturated aqueous sodium chloride solution
3. 3
   أخرىdried
4. 4
   ترشيحfiltered
5. 5
   أخرىThe solvent is removed in vacuo
6. 6
   أخرىthe residue is purified by preparative HPLC with addition of small portions of aqueous hydrochloric acid
7. 7
   أخرى25 mg (42% of theory) of the product are obtained

الإجراء التجريبي

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.

المصدر