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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1891697Generated: October 31, 2026

Tetrahydrofuran → 3-(3-(4-Phenylamino-benzyl)-isoxazol-5-yl)-pyridin-2-ylamine

https://huagongshe.com/reaction/1891697

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTetrahydrofuranHCID 8028—
ReactantTriethylamineHCID 8471—
Reactant3-Ethynylpyridin-2-amineHCID 12422526—
Reactant(4-Phenylamino-phenyl)-acetohydroximoyl chlorideHCID 72262877—
SolventWaterHCID 962—
Product3-(3-(4-Phenylamino-benzyl)-isoxazol-5-yl)-pyridin-2-ylamineHCID 5925528338.2%

Reaction Conditions

Temperature50 °C

Reaction Steps

To a tetrahydrofuran (3 mL) solution of (4-phenylamino-phenyl)-acetohydroximoyl chloride (150 mg, 0.576 mmol) described in Manufacturing Example 69-1-4 and 3-ethynyl-pyridin-2-ylamine (43 mg, 0.367 mmol) described in Manufacturing Example 1-2-3 was added triethylamine (201 μL, 1.44 mmol) at room temperature, which was stirred for 7 hours at 50° C. Water was added to the reaction solution at room temperature, which was then extracted with ethyl acetate. The organic layer was washed with water and saturated aqueous sodium chloride, and dried over anhydrous magnesium sulfate. The solvent was evaporated under a reduced pressure. The residue was purified by NH silica gel column chromatography (heptane:ethyl acetate=4:1-2:1) to obtain the title compound (48 mg, 24%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08507530B2
Source datasetuspto-grants-2013_08
ORD IDord-44e1be6aa2104997b2f8ab7d26d98ed1
Source noteuspto-grants-2013_08