Hydrochloric Acid → HCID 178490240, compound

Participants

Reaction Steps

In 50 ml of a 50% aqueous solution of dioxane was dissolved 0.5 g of (S,S)-3-(3-aminopropyl)-4-[2-benzyloxycarbonylamino-3-(4-methoxyphenyl)propionyl1-2-oxopiperazine-1-acetic acid produced in Reference Example 35. To the solution was added 0.24 g of NaHCO3, to which was then added 0.377 g of 4-guanidinobenzoic acid 3,5-dioxo-4-azatricyclo[5,2,1,0 2,6)deca-8-en-4-yl ester hydrochloride. The mixture was stirred for two hours at room temperature. The pH of the reaction mixture was adjusted to 3 with 1N-HCl, followed by distilling off dioxane. The residue was purified by means of a column chromatography (eluting with H2O→10% aqueous solution of CH3CN→a 20% aqueous solution of CH3CN→a 50% aqueous solution of CH3CN) to afford 0.43 g of the title compound.

Provenance & Evidence