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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1631164Generated: November 4, 2026

Water → 2-[2-Amino-4-(1,3-dihydroisoindole-2-carbonyl)quinazolin-6-yl]-4,5-difluorobenzyl 2,2-dimethylpropionate

https://huagongshe.com/reaction/1631164

Reaction equation

Participants

RoleNameHCIDCharge
ReactantWaterHCID 962—
ReactantEthyl AcetateHCID 8857—
ReactantPivaloyl chlorideHCID 62493—
Reactant[2-Amino-6-[4,5-difluoro-2-(hydroxymethyl)phenyl]quinazolin-4-yl]isoindolin-2-ylmethanoneHCID 56943446—
Catalyst4-(Dimethylamino)pyridineHCID 14284—
SolventDimethylformamideHCID 6228—
Product2-[2-Amino-4-(1,3-dihydroisoindole-2-carbonyl)quinazolin-6-yl]-4,5-difluorobenzyl 2,2-dimethylpropionateHCID 56943974—

Reaction Conditions

Temperature80 °C

Reaction Steps

47 μl of pivaloyl chloride are added to a solution of 200 mg of [2-amino-6-(4,5-difluoro-2-hydroxymethylphenyl)quinazolin-4-yl]-(1,3-dihydroisoindol-2-yl)methanone and 2 mg of 4-(dimethylamino)pyridine (DMAP) in 4 ml of dimethylformamide, and the mixture is stirred at 80° C. for 16 h. 8 ml of ethyl acetate and 8 ml of water are added, the organic phase is separated off and evaporated to dryness in vacuo. The residue is dissolved in 1 ml of dimethyl sulfoxide and purified by chromatography (reversed phase HPLC).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08791129B2
Source datasetuspto-grants-2014_07
ORD IDord-592c3d3d4cf6472ab893848fe720b6ac
Source noteuspto-grants-2014_07