Dicyclohexylcarbodiimide → HCID 14697224, compound

Participants

Reaction Steps

5-Aminomethyl-2-n-butyl-1-[(2'-carbomethoxybiphenyl-4-yl)methyl]-4-chloroimidazole (prepared by the procedure of Example 148, Part C, in EP No. 0253310) (0.71 g, 1.7 mmol), 1 eq), 4-[3-(N-t-butoxycarbonyl-N-isopropylamino)-2-hydroxypropoxy]indole-2-carboxylic acid (prepared by the procedure of Example 1, Part g, in EPO No. 174162) (0.84 g, 1.7 mmol, 1 eq), 1-hydroxybenzotriazole (0.24 g, 1.8 mmol, 1.05 eq), dicyclohexylcarbodiimide (0.37 g, 1.8 mmol, 1.05 eg) and DMF (25 mL) were mixed at 0° C. and left in the refrigerator for 4 days at that temperature. The dicyclohexylurea was filtered off and the mixture concentrated and chromatographed in 1:1 hexane/ethyl acetate yielding 970 mg of a white solid; mp 157.5°-160° C.

Provenance & Evidence