Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1406324Generated: October 31, 2026

Potassium Carbonate → 1-(6-amino-3'-fluoro-5-{(1R)-1-[5-fluoro-2-(2H-1,2,3-triazol-2-yl)phenyl]ethoxy}-3,4'-bipyridin-2'-yl)azetidin-3-ol

https://huagongshe.com/reaction/1406324

Reaction equation

Participants

RoleNameHCIDCharge
ReactantPotassium CarbonateHCID 11430—
Reactant3-Hydroxyazetidine hydrochlorideHCID 2759290—
Reactant2',3'-difluoro-5-{(1R)-1-[5-fluoro-2-(2H-1,2,3-triazol-2-yl)phenyl]ethoxy}-3,4'-bipyridin-6-amineHCID 67466925—
SolventDimethyl SulfoxideHCID 679—
Product1-(6-amino-3'-fluoro-5-{(1R)-1-[5-fluoro-2-(2H-1,2,3-triazol-2-yl)phenyl]ethoxy}-3,4'-bipyridin-2'-yl)azetidin-3-olHCID 5458854330%

Reaction Steps

2′,3′-Difluoro-5-[(R)-1-(5-fluoro-2-[1,2,3]triazol-2-yl-phenyl)-ethoxy-[3,4′]bipyridinyl-6-ylamine (example 129) (35 mg, 0.085 mmol, 1.0 eq) and potassium carbonate (115 mg, 0.833 mmol, 9.8 eq) and 3-hydroxyazetidine hydrochloride (91.3 mg, 0.833 mmol, 9.8 eq) in anhydrous DMSO (2 mL) were microwaved for 10 min. at 150° C. The mixture was filtered, concentrated, and purified with a reverse phase pre-HPLC under acidic condition to give the title compound (11.8 mg, 30% yield) as a amorphous solid after lyophilization.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08916593B2
Source datasetuspto-grants-2014_12
ORD IDord-97ad367bd4c4492ea651ceb533b61456
Source noteuspto-grants-2014_12