1-Methylpiperazine → N-[5-(4-methylpiperazin-1-yl)pyrazin-2-yl]acetamide

温度

120 °C

1-methylpiperazine (2.318 g, 23.14 mmol), N-(5-bromopyrazin-2-yl)acetamide (1 g, 4.63 mmol), tri-tert-butylphosphine (1.873 g, 9.26 mmol), tris(dibenzylideneacetone)dipalladium (0.085 g, 0.09 mmol) and potassium 2-methylpropan-2-olate (1.039 g, 9.26 mmol) were suspended in DMF (9.26 ml) and sealed into a microwave tube. The reaction was heated to 120 °C for 40 minutes in the microwave reactor and cooled to RT. The mixture was diluted with methanol and acidified with HCl, then the solution was purified by ion exchange chromatography, using an SCX column. The desired product was eluted from the column using 7M NH3/MeOH and pure fractions were evaporated to dryness to afford N-(5-(4-methylpiperazin-1-yl)pyrazin-2-yl)acetamide (0.866 g, 80 %) as a dark oil. Used without further purification.

ORDレコード

ord-96727602adb24b28af9c737e24f7315c

出典データセット

750 AstraZeneca ELN dataset

元リンク

出典を表示