Reaktion #325192

Reaktionsgleichung

3-(3-fluoro-5-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

K2CO3

Iodocyclopentane

→

1-cyclopentyl-3-(3-fluoro-5-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   Sonstigereaction
2. 2
   Sonstigereaction
3. 3
   workup.STIRRINGwas stirred for 2 hours
4. 4
   SonstigeSolid K2CO3 was removed by filtration
5. 5
   SonstigeSolvent was partially removed in vacuo
6. 6
   workup.ADDITIONSodium citrate (50 ml) was added
7. 7
   Sonstigereaction
8. 8
   Extraktionwas extracted with EtOAc
9. 9
   EinengenOrganic phases concentrated in vacuo
10. 10
    Sonstigepurified
11. 11
    Sonstigeto yield BA79

Vorschrift

3-(3-fluoro-5-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine (BA75, 100 mg, 0.386 mmol) was dissolved in DMF (10 ml). K2CO3 (250 mg, 1.54 mmol) was added and reaction was stirred at room temperature under an argon atmosphere. Iodocyclopentane (0.134 ml, 1.16 mmol) was added with a syringe and reaction was stirred for 2 hours. Solid K2CO3 was removed by filtration. Solvent was partially removed in vacuo. Sodium citrate (50 ml) was added and reaction was extracted with EtOAc. Organic phases concentrated in vacuo and purified using by RP-HPLC (MeCN:H2O:0.1% TFA) to yield BA79.

Quelle