反应详情

To a mixture comprising 3,5-diamino-6-chloro-pyrazine-2-carboxylic acid (2-methylamino-ethyl)-amide (Intermediate E) (0.5 g, 2.0 mmol) and 4-(Boc-amino)butyl bromide (0.8 g, 3.1 mmol) in DMF (5 mL) is added sodium carbonate (0.4 g, 4.0 mmol). The resulting mixture is heated at reflux for 3 h and then allowed to cool to RT, filtered and concentrated in vacuo. The crude product is dissolved in DCM and filtered to remove any undissolved impurities. The filtrate is concentrated in vacuo to yield the title compound which is used in the next step without further purification.

1. temperatureThe resulting mixture is heated
2. temperatureat reflux for 3 h
3. filtrationfiltered
4. concentrationconcentrated in vacuo
5. dissolutionThe crude product is dissolved in DCM
6. filtrationfiltered
7. customto remove any undissolved impurities
8. concentrationThe filtrate is concentrated in vacuo