تفاعل #172257

معادلة التفاعل

1-Benzenesulfonyl-5-bromo-2-methyl-1H-pyrrolo[2,3-b]pyridine

4-((4-methylpiperazin-1-yl)methyl)phenylboronic acid

sodium carbonate

→

title compound

المردود 74.1%

2-methyl-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine

المردود 74.1%

المذيبات

water

acetonitrile

ظروف التفاعل

المعالجة

1. 1
   أخرىthe mixture is irradiated for 5 minutes at 150 degrees in a Biotage microwave reactor
2. 2
   درجة الحرارةAfter cooling
3. 3
   استخلاصextracted with ethyl acetate
4. 4
   أخرىdried
5. 5
   تركيزconcentrated
6. 6
   غسيلMPLC silica gel chromotagraphy 5-20% MeOH in dichloromethane gradient elution

الإجراء التجريبي

1-Benzenesulfonyl-5-bromo-2-methyl-1H-pyrrolo[2,3-b]pyridine (378 mg, 1.076 mmole) and 4-((4-methylpiperazin-1-yl)methyl)phenylboronic acid (303 mg, 1.29 mmole) are dissolved in acetonitrile (10 mL) and treated with 10 mL 1 M sodium carbonate solution. To this is added 40 mg of PdCl2(PPh3)2 catalyst, and the mixture is irradiated for 5 minutes at 150 degrees in a Biotage microwave reactor. After cooling, the reaction mixture is diluted with water and extracted with ethyl acetate, dried, and concentrated. MPLC silica gel chromotagraphy 5-20% MeOH in dichloromethane gradient elution, provided 367 mg of the title compound as a solid.

المصدر