1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 11533845, compound

Participants

Reaction Steps

The compound of Example 45 (100 mg) was suspended in 2 mL of methylene chloride. To the suspension were added 34 μL of N-methylpiperazine, 79 mg of WSC and 72 μL of diisopropyl-ethylamine, and the mixture was stirred at room temperature overnight. To the reaction mixture was added brine, the mixture was extracted with ethyl acetate. The organic layer was washed with brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The residue was purified by chromatography on silica gel (chloroform-methanol-28% aqueous ammonia=100:10:1) to give 95 mg of N-[4-(6-amino-5-cyano-2-{6-[3-(4-methylpiperazin-1-yl)-3-oxopropyl]pyridin-2-ylmethylsulfanyl}pyrimidin-4-yl)phenyl]-acetamide.

Provenance & Evidence