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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2035670Generated: October 31, 2026

Hydrochloric Acid → 2-([1,2,4]Triazolo[4,3-a]pyridin-3-yl)-6-fluoro-8-(trans-5-fluoroazepan-4-yloxy)quinoline

https://huagongshe.com/reaction/2035670

Reaction equation

Participants

RoleNameHCIDCharge
ReactantHydrochloric AcidHCID 313—
Reactanttrans-Tert-butyl 4-(2-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-6-fluoroquinolin-8-yloxy)-5-fluoroazepane-1-carboxylateHCID 131731016—
SolventChloroformHCID 6212—
Product2-([1,2,4]Triazolo[4,3-a]pyridin-3-yl)-6-fluoro-8-(trans-5-fluoroazepan-4-yloxy)quinolineHCID 67233623—

Reaction Steps

Enantiomer 1 of trans-tert-butyl 4-(2-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-6-fluoroquinolin-8-yloxy)-5-fluoroazepane-1-carboxylate (Peak 1 from Example 91, Step E; 0.210 g, 0.424 mmol) was dissolved in CHCl3 (4.3 mL). To this solution was added HCl (4.24 mL, 17.0 mmol, 4.0M Dioxane) and the mixture was stirred at ambient temperature for 3 hours. The mixture was filtered through a polypropylene filter and washed with CH2Cl2 and Et2O, slurried in hexanes and then dried carefully in vacuo to provide the desired product as white solid. MS ESI (+) m/z 396.1 (M+1) detected.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08575145B2
Source datasetuspto-grants-2013_11
ORD IDord-09aeecba72df49499e7906347eeffc09
Source noteuspto-grants-2013_11