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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 588254Generated: October 30, 2026

Picolinic acid → HCID 66653896, compound

https://huagongshe.com/reaction/588254

Reaction equation

Participants

RoleNameHCIDCharge
ReactantPicolinic acidHCID 1018—
Reactant2,3-DimethyliodobenzeneHCID 141645—
ReactantHCID 67032456HCID 67032456—
CatalystCopper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI)HCID 24350—
SolventDimethyl SulfoxideHCID 679—
SolventSodium chloride; waterHCID 57417360—
ProductHCID 66653896HCID 6665389693.1%

Reaction Conditions

Temperature90 °C

Reaction Steps

To a degassed solution of 3-[2-(4-hydroxy-phenyl)-2-methyl-morpholin-4-yl]-propionic acid tert-butyl ester (1.07 g; 3.33 mmol), and 3-iodo-o-xylene (0.97 g; 4.16 mmol) in DMSO (20 mL) was added picolinic acid (82 mg; 0.67 mmol), CuI (63.4 mg; 0.33 mmol) and powdered (1.41 g; 6.66 mmol). The resulting mixture was heated for 24 h, at 90° C. After cooling to room temperature, brine was added and the mixture extracted with CH2Cl2. The combined layers were dried (Na2SO4), filtered, and concentrated in vacuo. The residue was purified by column chromatography (SiO2, Et2O/hexanes 1:1) to afford 3-{2-[4-(2,3-dimethyl-phenoxy)-phenyl]-2-methyl-morpholin-4-yl}-propionic acid tert-butyl ester (1.32 g).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09227960B2
Source datasetuspto-grants-2016_01
ORD IDord-eaa9635784b841049bbe869c80e807ca
Source noteuspto-grants-2016_01