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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1162612Generated: October 29, 2026

1-(4-Amino-3-fluorophenyl)pyridin-2-one → 5-chloro-thiophene-2-carboxylic acid ((R)-1-{1-[2-fluoro-4-(2-oxo-pyridin-1-yl)-phenylcarbamoyl]-ethyl}-pyrrolidin-3-yl)-amide

https://huagongshe.com/reaction/1162612

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1-(4-Amino-3-fluorophenyl)pyridin-2-oneHCID 22181548—
Reactant2-{(R)-3-[(5-chloro-thiophene-2-carbonyl)-amino]-pyrrolidin-1-yl}-propionic acid ethyl esterHCID 58748289—
Product5-chloro-thiophene-2-carboxylic acid ((R)-1-{1-[2-fluoro-4-(2-oxo-pyridin-1-yl)-phenylcarbamoyl]-ethyl}-pyrrolidin-3-yl)-amideHCID 58748343—

Reaction Steps

6.4 Using general procedure F 2-{(R)-3-[(5-chloro-thiophene-2-carbonyl)-amino]-pyrrolidin-1-yl}-propionic acid ethyl ester was reacted with 1-(4-amino-3-fluoro-phenyl)-1H-pyridin-2-one (CAS 536747-52-1, prepared according to WO 2003045912) to give 5-chloro-thiophene-2-carboxylic acid ((R)-1-{1-[2-fluoro-4-(2-oxo-pyridin-1-yl)-phenylcarbamoyl]-ethyl}-pyrrolidin-3-yl)-amide. Yellow solid. MS 487.4 ([M−H]−)

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07820699B2
Source datasetuspto-grants-2010_10
ORD IDord-16fb5fc165ed4d28bb8077d445fd63f7
Source noteuspto-grants-2010_10