1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 5-({[(4-methoxy-2,6-dimethylphenyl)sulfonyl](methyl)amino}methyl)-N-(1,2,2,6,6-pentamethylpiperidin-4-yl)furan-3-carboxamide

Participants

Reaction Steps

5-({[(4-Methoxy-2,6-dimethylphenyl)sulfonyl](methyl)amino}methyl)furan-3-carboxylic acid (53 mg, 0.15 mmol) was dissolved in DMF (1 mL) and HOBt (23 mg, 0.15 mmol) and EDCI (29 mg, 0.15 mmol) were added. The reaction was stirred for 1 h prior to addition of 2,2,6,6-tetramethylpiperidin-4-amine (21 mg, 0.135 mmol). The reaction was stirred for 16 h and then absorbed directly on to Isolute SCX-2 cartridge, washed with MeOH (5 mL) and then eluted with 7 N NH3 in MeOH (5 mL). The solvent was removed under a stream of N2 and the resulting crude product purified using prep method A.

Provenance & Evidence