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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1411072Generated: October 31, 2026

Hydrochloric Acid → HCID 68297233, compound

https://huagongshe.com/reaction/1411072

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHydrochloric AcidHCID 313—
ReactantEthyl AcetateHCID 8857—
Reactant3-(Tributylstannyl)pyridineHCID 3483848—
Reactant1-Benzyl-8-bromo-5-hydroxy-2-oxo-3-(2-trifluoromethyl-phenyl)-1,2-dihydro-[1,7]naphthyridine-6-carboxylic acid methyl esterHCID 86714184—
CatalystHCID 178418476HCID 178418476—
SolventDimethylformamideHCID 6228—
SolventSodium chloride; waterHCID 57417360—
ProductHCID 68297233HCID 6829723337.6%

Reaction Conditions

Temperature120 °C

Reaction Steps

A mixture of 1-benzyl-8-bromo-5-hydroxy-2-oxo-3-(2-trifluoromethyl-phenyl)-1,2-dihydro-[1,7]naphthyridine-6-carboxylic acid methyl ester (80 mg, 0.15 mmol), 3-tributylstannanyl-pyridine (0.072 mL, 0.23 mmol) and PdCl2(PPh3)2 (21 mg, 0.030 mmol) in 4 mL of DMF was heated at 120° C. for 2 h under nitrogen atmosphere. After the mixture was cooled to r.t., EtOAc and brine were added. 1 M HCl was added until pH was about 3. The aqueous layer was extracted with additional EtOAc, and the combined organic layer was washed with water and dried over MgSO4. After evaporating the solvent in vacuo, the crude product was purified by silica gel chromatography (5-100% EtOAc/hexanes+1% AcOH) to give 30 mg of the title compound. MS: (+) m/z 532.37 (M+1).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08921389B2
Source datasetuspto-grants-2014_12
ORD IDord-62e4f41e01a6495787e017122c41fb18
Source noteuspto-grants-2014_12