6-Isocyanato-2,3-dihydro-1,4-benzodioxine → N-(2-t-Butoxycarbonylaminophenyl)-4-[3-(2,3-dihydrobenzo[1,4]dioxin-6-yl)-1-[3-(4-methylpiperazin-1-yl)propyl]ureidomethyl]benzamide

Participants

Reaction Steps

2,3-Dihydrobenzo[1,4]dioxin-6-ylisocyanate (0.11 mL, 0.80 mmol) was added to a solution of N-(2-t-butoxycarbonylaminophenyl)-4-[3-(4-methylpiperazin-1-yl)propylaminomethyl]benzamide (Reference Compound No. 4-1, 350 mg, 0.73 mmol) in anhydrous dichloromethane (15 mL), and then the reaction mixture was stirred at room temperature for 40 minutes. The reaction mixture was concentrated under reduced pressure, and then the residue was purified by silica gel column chromatography (chloroform-methanol) to give 460 mg of the title reference compound as a colorless amorphous product. (Yield 94%)

Provenance & Evidence