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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 251864Generated: October 30, 2026

Acrylamide → 7-[(3RS,5SR)-4-(3-Amino-3-oxopropyl)-3,5-dimethylpiperazin-1-yl]-6-fluoro-8-methoxy-N-[2-methyl-4-(trifluoromethoxy)benzyl]-4-oxo-1-(2,2,2-trifluoroethyl)-1,4-dihydroquinoline-3-carboxamide

https://huagongshe.com/reaction/251864

Reaction equation

Participants

RoleNameHCIDCharge
ReactantAcrylamideHCID 6579—
ReactantLithium perchlorateHCID 23665649—
Reactant7-[(3RS,5SR)-3,5-Dimethylpiperazin-1-yl]-6-fluoro-8-methoxy-N-[2-methyl-4-(trifluoromethoxy)benzyl]-4-oxo-1-(2,2,2-trifluoroethyl)-1,4-dihydroquinoline-3-carboxamideHCID 72493844—
CatalystAcetonitrileHCID 6342—
SolventDimethyl SulfoxideHCID 679—
Product7-[(3RS,5SR)-4-(3-Amino-3-oxopropyl)-3,5-dimethylpiperazin-1-yl]-6-fluoro-8-methoxy-N-[2-methyl-4-(trifluoromethoxy)benzyl]-4-oxo-1-(2,2,2-trifluoroethyl)-1,4-dihydroquinoline-3-carboxamideHCID 72493816—

Reaction Conditions

Temperature70 °C

Reaction Steps

A few drops of acetonitrile are added at room temperature to 55 mg of the compound of Example 52, 18 mg of acrylamide and 35 mg of lithium perchlorate, so that a stirrable suspension results. The mixture is heated to 70° C. over night and left to cool. After the addition of DMSO the whole mixture is separated by preparative HPLC (Method 5). After concentrating the suitable fractions and drying under high vacuum 30 mg (40% of theory) of the title compound are obtained.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07867992B2
Source datasetuspto-grants-2011_01
ORD IDord-0b93aa94662c4e62b1e0a9feeacf9e77
Source noteuspto-grants-2011_01