Triethylamine → Phthalimide

Participants

Reaction Steps

In a similar manner to Step 2 of Example 1, (E)-3-amino-4-(2-methoxycarbonylvinyl)-6-bromophthalimide (100 mg, 0.308 mmol) was dissolved in acetonitrile (7 mL), and the solution was treated with Compound BB (292 mg, 0.616 mmol), palladium acetate (5.5 mg, 0.025 mmol), tri(o-tolyl)phosphine (15 mg, 0.049 mmol) and triethylamine (0.429 mL, 3.08 mmol), followed by purification by preparative thin-layer chromatography (chloroform/acetonitrile=6/1) to obtain (E)-3-amino-4-(2-methoxycarbonylvinyl)-6-(tert-butoxycarbonyl)-5-[4-(tert-butoxycarbonyl)piperazin-1-ylcarbonyl]indol-2-yl)phthalimide (102 mg, yield 49%).

Provenance & Evidence