1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 10093336, compound

Participants

Reaction Steps

To a solution of 4-[2-fluoro-3-carboxyphenoxy]-5-(1-methylethyl)pyrrolo[2,1-f][1,2,4]triazine-6-carboxylic acid, ethyl ester (14 mg, 0.036 mmol) in dimethyl formamide at RT were added EDCI (14 mg, 0.07 mmol), DIPEA (20 μL, 0.11 mmol), HOBt (9.7 mg, 0.07 mmol), and methoxylamine hydrochloride (6 mg, 0.07 mmol). After stirring overnight, HPLC analysis revealed that only 10% product was formed. BOP reagent (0.1 mmol) was added. After 6 h, all the starting material was consumed. The mixture was purified by reverse phase preparative HPLC to afford the desired product (14 mg, 93%). LC/MS: (M+H)+=417.

Provenance & Evidence