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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 84872Generated: October 29, 2026

Acetic Acid → (R)-4-(2-amino-1-cyclopropyl-2-oxoethylamino)-5-fluoro-2-(3-methylisothiazol-5-ylamino)benzamide

https://huagongshe.com/reaction/84872

Reaction equation

Participants

RoleNameHCIDCharge
ReactantAcetic AcidHCID 176—
ReactantHydrogen PeroxideHCID 784—
ReactantSodium HydroxideHCID 14798—
Reactant(R)-2-(4-cyano-2-fluoro-5-(3-methylisothiazol-5-ylamino)phenylamino)-2-cyclopropylacetamideHCID 67508988—
SolventDimethyl SulfoxideHCID 679—
SolventEthanolHCID 702—
Product(R)-4-(2-amino-1-cyclopropyl-2-oxoethylamino)-5-fluoro-2-(3-methylisothiazol-5-ylamino)benzamideHCID 67511164—

Reaction Steps

To a solution of (R)-2-(4-cyano-2-fluoro-5-(3-methylisothiazol-5-ylamino)phenylamino)-2-cyclopropylacetamide (38 mg, 0.110 mmol) in EtOH (1 mL) and DMSO (0.5 mL), aq. 1N NaOH (0.5 mL, 0.50 mmol) and aq. H2O2 (50%, 0.5 mL) were added. The mixture was stirred at room temperature for 20 min. HOAc (0.5 mL) was added. The mixture was purified by HPLC to give the titled compound (18 mg). MS 364.2 (M+H); UV 219.3, 280.5, 302.6 nm.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08846928B2
Source datasetuspto-grants-2014_09
ORD IDord-5063b3a9aa404d36ad073fd4f476be74
Source noteuspto-grants-2014_09