Ethylmorpholine → HCID 86749862, compound

Participants

Reaction Steps

0.8 g of (RS)-(4-tert-butoxycarbonylmethyl-1-butylsulphonyl-3-oxo-piperazin-2-yl)-acetic acid is dissolved in 15 ml of DMF, treated in succession with 1.3 ml of 4-ethylmorpholine, 0.92 g of BOP and 0.72 g of (S)-1-amidino-3-(aminomethyl)-piperidine dihydrochloride. The reaction mixture is stirred at room temperature overnight, then evaporated and the residue is chromatographed on RP-18 with a water-acetonitrile gradient. The product fractions are evaporated and filtered over an ion exchanger (Cl- form) with water-ethanol. Colourless [3-[(S)-1-(amino-imino-methyl)-piperidin-3-ylmethylcarbamoylmethyl]-4-butylsulphonyl-2-oxo-piperazin-1yl]acetic acid (1:1), MS (ion spray): 475.6 (M+H)+, is isolated after evaporation.

Provenance & Evidence