Hydrochloric Acid → HCID 58748169, compound

Participants

Reaction Steps

A solution of 394 mg (2S,4R)-4-[(5-chloro-thiophene-2-carbonyl)-amino]-1-{[2-fluoro-4-(2-oxo-pyridin-1-yl)-phenylcarbamoyl]-methyl}-pyrrolidine-2-carboxylic acid methyl ester (example 11.4) in 10 ml THF was treated with 1.5 ml 1N NaOH. The reaction mixture was stirred for 4 hrs at r.t., then brought to pH 7 with 3N HCl and concentrated. The crude product was purified by chromatography (silica gel; CH2Cl2/MeOH 4:1, then MeOH). The product-containing fractions were concentrated, triturated with water and dried to give 290 mg (2S,4R)-4-[(5-chloro-thiophene-2-carbonyl)-amino]-1-{[2-fluoro-4-(2-oxo-pyridin-1-yl)-phenylcarbamoyl]-methyl}-pyrrolidine-2-carboxylic acid as an off-white solid. MS 519.3 ([M+H]+)

Provenance & Evidence