1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → HCID 66631721, compound

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Reaction Steps

2-(4-tert-Butoxycarbonylamino-benzoylamino)-3-(4-cyano-3-fluoro-phenyl)-propionic acid ethyl ester. EDCI (560 mg, 2.92 mmol) was added to a solution of 4-tert-butoxycarbonylamino-benzoic acid (661 mg, 2.7 mmol) in dry CH2Cl2 (5 mL). After the mixture was stirred for 0.5 hr, 2-amino-3-(4-cyano-3-fluoro-phenyl)-propionic acid ethyl ester (627 mg, 2.66 mmol) was added and the mixture was stirred for another 5 hrs at room temperature. The mixture was partitioned between EtOAc and water. The combined organic layers were washed with brine, dried over anhydrous Na2SO4, concentrated under reduced pressure, and purified by silica gel chromatography to give the title compound as a white solid (906 mg, 75% yield).

Provenance & Evidence