반응 #715633

반응 방정식

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

cyclopropylmethylamine

Cs2CO3

water

→

6-Benzyl-N-(cyclopropylmethyl)-1,7-dimethyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyridin-4-amine

용매

N-methylpyrrolidinone

반응 조건

후처리

1. 1
   기타was degassed
2. 2
   여과after which time the reaction mixture was filtered
3. 3
   기타the product was purified by preparative HPLC-MS (Waters XBridge C18
4. 4
   세척eluting with a gradient of MeCN/H2O containing 0.15% NH4OH)

실험 절차

A suspension of 6-benzyl-4-chloro-1,7-dimethyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyridine (20.0 mg, 0.0644 mmol, from Step 7), cyclopropylmethylamine (51 μL, 0.60 mmol, Aldrich), tBuBrettPhos Pd G3 (6.5 mg, 0.0076 mmol, Aldrich) and Cs2CO3 (0.045 g, 0.14 mmol) in N-methylpyrrolidinone (0.3 mL) and water (0.030 g) was degassed and heated at 100° C. for 4.5 h, after which time the reaction mixture was filtered and the product was purified by preparative HPLC-MS (Waters XBridge C18, eluting with a gradient of MeCN/H2O containing 0.15% NH4OH). Yield: (10.5 mg, 47%).

출처