Reaktion #2283855

Reaktionsgleichung

MeCN water

2,6-difluoro-N-(2-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)-3-(propylsulfonamido)benzamide

1-methyl-1H-indol-5-ylboronic acid

K2CO3

→

2,6-difluoro-N-(2-(1-methyl-1H-indol-5-yl)-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)-3-(propylsulfonamido)benzamide

Ausbeute 70.0%

Lösungsmittel

EtOAc water

Reaktionsbedingungen

Aufarbeitung

1. 1
   Filtrationfiltered through GF/F paper
2. 2
   Sonstigethe layers were separated
3. 3
   TrocknenThe organic layer was dried over MgSO4
4. 4
   Filtrationfiltered
5. 5
   Einengenconcentrated

Vorschrift

A mixture of 2,6-difluoro-N-(2-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)-3-(propylsulfonamido)benzamide (27 mg, 40 mmol, 1.0 eq.), 1-methyl-1H-indol-5-ylboronic acid (1.5 eq.), K2CO3 (20 eq.) and Pd(PPh3)4 (0.05 eq.) were taken up in 4:1 MeCN/water (0.7 mL) and heated to 160° C. for 15 minutes under microwave irradiation. The mixture was diluted with 1:1 EtOAc/water (6 mL), filtered through GF/F paper, and the layers were separated. The organic layer was dried over MgSO4, filtered, and concentrated to afford 2,6-difluoro-N-(2-(1-methyl-1H-indol-5-yl)-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)-3-(propylsulfonamido)benzamide (19 mg, 70%).

Quelle