Reaktion #715617

Reaktionsgleichung

6-benzyl-4-chloro-1,7-dimethyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyridine

ethanolamine

Cs2CO3

→

2-[(6-Benzyl-1,7-dimethyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyridin-4-yl)amino]ethanol

Lösungsmittel

MeCN

NMP

Water

Reaktionsbedingungen

Aufarbeitung

1. 1
   TemperaturUpon cooling
2. 2
   Filtrationfiltered
3. 3
   Sonstigepurified via preparative HPLC-MS (Waters XBridge C18
4. 4
   Wascheneluting with a gradient of MeCN/H2O containing 0.15% NH4OH)

Vorschrift

A degassed mixture of 6-benzyl-4-chloro-1,7-dimethyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyridine (25.0 mg, 0.0804 mmol, Example 228, Step 7), ethanolamine (44 mg, 0.72 mmol, Aldrich), Cs2CO3 (79 mg, 0.24 mmol, Aldrich) and tBuBrettPhos Pd G3 (8.2 mg, 0.0096 mmol, Aldrich) in NMP (1 mL) and Water (38 μL) was heated at 100° C. overnight. Upon cooling, the reaction mixture was diluted with MeCN, filtered and purified via preparative HPLC-MS (Waters XBridge C18, eluting with a gradient of MeCN/H2O containing 0.15% NH4OH). Yield: (5.9 mg, 22%).

Quelle