1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 9805501, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 3-methoxy-4-(5,6-dichloro-1H-indol-2-yl)-benzoic acid (0.15 g, 0.45 mmol), WSC (0.094 g, 0.5 mmol), HOAT (0.067 g, 0.5 mmol), 4-amino-1,2,2,6,6-pentamethylpiperidine (0.15 g, 0.9 mmol) in DMF (2 ml) was stirred at 50° C. for 18 h. The mixture was then poured in a large volume of water and extracted with AcOEt. The organic phase was washed with water, dried over MgSO4 and concentrated in vacuo. The residue was purified by flash chromatography (SiO2; CH2Cl2—MeOH—NH4OH: 91.5-7.5-1) then crystallised in di-isopropyl ether to afford 0.13 g (0.26 mmol. yield 59%) of the title compound, mp=260° C.

Provenance & Evidence