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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2201104Generated: 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/2201104

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 numberUS09359375B2
Source datasetuspto-grants-2016_06
ORD IDord-b25a5026ed604006b07985503f7ecec1
Source noteuspto-grants-2016_06