Cyclopropylamine → HCID 11503850, compound

Participants

Reaction Steps

rac-4-{[(4-Chloro-benzenesulfonyl)-(2-oxo-azepan-3-yl)-amino]-methyl}-benzoic acid (0.70 g, 1.6 mmol) was dissolved in DMF and activated with the coupling reagent TPTU (0.48 g, 1.6 mmol) and Hünig's base (0.55 ml, 3.2 mmol) for 2 min. ⅛ of this activated mixture was delivered to a reaction tube on a parallel synthesizer containing cyclopropylamine (0.013 g, 0.22 mmol) and a further amount of Hünig's base (0.04 ml, 0.22 mmol) in DMF (3 ml). The reaction mixture was shaken for 2 h, concentrated under reduced pressure and purified directly using preparative RP(C18) chromatography: lyophilisate 40 mg; MS: m/e=476.1 (MH+), 493.1 (MNH4+).

Provenance & Evidence