Reaktion #1607378

Reaktionsgleichung

N-(4-(1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-methylthiazol-2-yl)-6-iodopyridin-2-amine

Na2CO3

→

N-(6-iodopyridin-2-yl)-5-methyl-4-(1H-pyrazol-4-yl)thiazol-2-amine

Ausbeute 34.0%

Lösungsmittel

TFA

Reaktionsbedingungen

Aufarbeitung

1. 1
   Extraktionthe aqueous phase was extracted with DCM
2. 2
   TrocknenThe organic phase was dried over MgSO4
3. 3
   Filtrationwas filtered
4. 4
   Einengenwas concentrated
5. 5
   SonstigeThe resulting crude product was purified by flash chromatography over silica gel

Vorschrift

According to Scheme 2 Step 5: A solution of N-(4-(1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-methylthiazol-2-yl)-6-iodopyridin-2-amine (0.27 mmol, 136 mg) in TFA (1.4 mL) was microwaved for 5 minutes at 140° C. The reaction mixture was neutralized with a saturated solution of Na2CO3 and the aqueous phase was extracted with DCM. The organic phase was dried over MgSO4, was filtered and was concentrated. The resulting crude product was purified by flash chromatography over silica gel using DCM/MeOH (100:0 to 90:10) as eluent to yield N-(6-iodopyridin-2-yl)-5-methyl-4-(1H-pyrazol-4-yl)thiazol-2-amine (91 μmol, 34 mg, 34%) as a white solid.

Quelle