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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 72468Generated: October 30, 2026

Hydrochloric Acid → 5-Chloro-2-(3-((2,4-difluorophenyl)amino)azetidin-1-yl)nicotinic acid

https://huagongshe.com/reaction/72468

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHydrochloric AcidHCID 313—
ReactantSodium HydroxideHCID 14798—
ReactantMethyl 5-chloro-2-(3-((2,4-difluorophenyl)amino)azetidin-1-yl)nicotinateHCID 67958025—
Solvent1,4-Dioxane--water (1/1)HCID 21886435—
Product5-Chloro-2-(3-((2,4-difluorophenyl)amino)azetidin-1-yl)nicotinic acidHCID 6795808099.1%

Reaction Conditions

Temperature60 °C

Reaction Steps

To a solution of methyl 5-chloro-2-(3-((2,4-difluorophenyl)amino)azetidin-1-yl)nicotinate (D85) (37 mg, 0.104 mmol) in a mixture 3:1 1,4-dioxane/water (4 ml), 1M NaOH (0.157 ml) was added and the resulting mixture was stirred 12 h at 60° C. After cooling the reaction mixture was acidified to pH 1 by addition of 1M HCl. The resulting precipitate was collected by filtration and afforded the title compound (D118) (35 mg).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08828987B2
Source datasetuspto-grants-2014_09
ORD IDord-eb0af1be355f463fbbdc1ec65a21a03d
Source noteuspto-grants-2014_09