3,4,5-Trimethoxybenzoic Acid → HCID 68681644, compound

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Reaction Steps

Experimental condition analogous to Example 13 were used with 2-[2-(2-Methyl-3-phenyl-allylamino)]-ethyl-(R) pyrrolidine-1-carboxylic acid tert-butyl ester (prepared from (R)-Pyrrolidine-1,2-dicarboxylic acid-1-tert-butyl ester according to the scheme 3) 0.6 g (2 mmol), 3,4,5-trimethoxy benzoic acid 0.51 g (2.4 mmol), O-(benzotriazole-1-yl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate 1.3 g (4 mmol) and triethylamine 0.2 ml. The intermediate 2-{2-[(2-methyl-3-phenyl-allyl)-(3,4,5-trimethoxy-benzoyl)-amino-]-ethyl}-pyrrolidine-1-carboxylic acid tert-butyl ester was dissolved in 10 ml of dioxane and 5 ml of 6 N HCl, yielding 0.35 g of the compound after basic work-up and purification. Yield: 39%.

Provenance & Evidence