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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2089639Generated: October 26, 2026

Dimethylformamide → 3-methoxy-2,2-dimethylpropionic acid 5-[[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylall yloxycarbonylimino]methyl}phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester

https://huagongshe.com/reaction/2089639

Reaction equation

Participants

RoleNameHCIDCharge
ReactantDimethylformamideHCID 6228—
ReactantTriethylamineHCID 8471—
ReactantCarbonic acid 2-methylallyl ester 4-nitrophenyl esterHCID 67469869—
Reactant3-methoxy-2,2-dimethylpropionic acid 5-[[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-carbamimidoylphen ylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester acetateHCID 67469945—
SolventWaterHCID 962—
SolventEthyl AcetateHCID 8857—
Product3-methoxy-2,2-dimethylpropionic acid 5-[[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylall yloxycarbonylimino]methyl}phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl esterHCID 6821286595.1%

Reaction Steps

A mixture of 3-methoxy-2,2-dimethylpropionic acid 5-[[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-carbamimidoylphen ylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester acetate (13 mg), triethylamine (0.0074 mL), carbonic acid 2-methylallyl ester 4-nitrophenyl ester (5.6 mg), and DMF (2 mL) was stirred for 3 days at room temperature. The resulting mixture was poured into ethyl acetate (100 mL) and water (30 mL). After shaking the mixture, the organic layer was collected, sequentially washed twice with water (30 mL) and with saturated aqueous sodium chloride solution (30 mL), and dried over anhydrous magnesium sulfate. The resulting mixture was filtered, and the filtrate obtained was concentrated under reduced pressure. The residue obtained was purified by NAM silica gel column chromatography (mixed solvent of methanol-ethyl acetate) to obtain the captioned compound (13 mg).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08436009B2
Source datasetuspto-grants-2013_05
ORD IDord-6455d7621b8f4b77aa4eb43a07109cc6
Source noteuspto-grants-2013_05