1-(4-Amino-3-fluorophenyl)pyridin-2-one → thiophene-2-carboxylic acid {(1S,2S,4R)-4-[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenylcarbamoyl]-2-hydroxy-cyclopentyl}-amide

Participants

Reaction Steps

In analogy to example 1C, 1R,3S,4S)-3-hydroxy-4-[(thiophene-2-carbonyl)-amino]-cyclo-pentanecarboxylic acid methyl ester was reacted with 1-(4-amino-3-fluoro-phenyl)-1H-pyridin-2-one (CAS 536747-52-1, prepared according to C. F. Bigge et al., patent application WO 2003045912) to give thiophene-2-carboxylic acid {(1S,2S,4R)-4-[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenylcarbamoyl]-2-hydroxy-cyclopentyl}-amide. Light yellow solid. MS: 442.1 ([M+H]+).

Provenance & Evidence