Triethylamine → 4-Chloro-5-methanesulfonyloxy-7-{1-(tert-butoxycarbonyl)-5-[4-(2-hydroxyethyl)pyperazin-1-ylmethyl]indol-2-yl}isoindolinone

Participants

Reaction Steps

In a similar manner to Step 1 of Example 289, 4-chloro-5-hydroxy-7-{1-(tert-butoxycarbonyl)-5-[4-(2-hydroxyethyl)pyperazin-1-ylmethyl]indol-2-yl}isoindolinone (62.5 mg, 0.0950 mmol) was dissolved in dichloromethane (2.4 mL), and the solution was treated with triethylamine (0.053 mL, 0.38 mmol) and methanesulfonyl chloride (0.015 mL, 0.019 mmol), followed by purification by slurry using hexane to obtain 4-chloro-5-methanesulfonyloxy-7-{1-(tert-butoxycarbonyl)-5-[4-(2-hydroxyethyl)pyperazin-1-ylmethyl]indol-2-yl}isoindolinone (50.1 mg, yield 72%).

Provenance & Evidence