反应详情

To a 25 ml one necked round bottom flask 2-cyano-N,N-dimethyl-3-(6-(7-pivaloyl-5-((2-(trimethylsilyl)ethoxy)methyl)-5H-pyrrolo[2,3-b]pyrazin-2-ylamino)pyridin-3-yl)acrylamide (0.1 g, 0.000182 mole) was taken in CH2Cl2 (10 ml). To this reaction mixture TFA (2.0 ml) was added dropwise at 0° C. After completion of the addition, the reaction mixture was warmed up to RT and then stirred for 16 hrs. After completion of the reaction, CH2Cl2 was distilled out and set pH 8 to 9 using saturated NaHCO3 solution (20.0 ml) at 5° C. Reaction mixture was stirred for 15 min. The solid was filtered, washed with methanol followed by n-pentane and dried under vacuum to yield 40 mg of 2-cyano-N,N-dimethyl-3-(6-(7-pivaloyl-5H-pyrrolo[2,3-b]pyrazin-2-ylamino)pyridin-3-yl)acrylamide.

1. additionAfter completion of the addition
2. distillationwas distilled out
3. customat 5° C
4. customReaction mixture
5. stirringwas stirred for 15 min
6. filtrationThe solid was filtered
7. washwashed with methanol
8. customdried under vacuum