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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2175000Generated: October 30, 2026

Trifluoroacetic acid → (1S,6R)-3,8-Diazabicyclo[4.2.0]octan-8-yl(2-fluoro-6-(2H-1,2,3-triazol-2-yl)phenyl)methanone

https://huagongshe.com/reaction/2175000

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant(1S,6R)-tert-Butyl 8-(2-fluoro-6-(2H-1,2,3-triazol-2-yl)benzoyl)-3,8-diazabicyclo[4.2.0]octane-3-carboxylateHCID 67086932—
SolventDichloromethaneHCID 6344—
Product(1S,6R)-3,8-Diazabicyclo[4.2.0]octan-8-yl(2-fluoro-6-(2H-1,2,3-triazol-2-yl)phenyl)methanoneHCID 67086546—

Reaction Steps

To (1S,6R)-tert-butyl 8-(2-fluoro-6-(2H-1,2,3-triazol-2-yl)benzoyl)-3,8-diazabicyclo[4.2.0]octane-3-carboxylate (400 mg, 1.0 mmol) in CH2Cl2 (5 mL) was added TFA (5 mL). After the reaction was judged complete, the volatiles were removed under reduced pressure. The resulting residue was neutralized using 5% Na2CO3(aq) followed by extraction with CH2Cl2 (3×). The combined organics were dried (Na2SO4) and concentrated to give the title compound as an oil that was used without further purification.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09062044B2
Source datasetuspto-grants-2015_06
ORD IDord-67e96bc5236a441db447d44ce039a747
Source noteuspto-grants-2015_06