Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 477832Generated: October 26, 2026

1,8-Diazabicyclo(5.4.0)undec-7-ene → 1-Ethyl-6,8-difluoro-7-[2-(formylaminomethyl)morpholino]-1,4-dihydro-4-oxoquinoline-3-carboxylic acid

https://huagongshe.com/reaction/477832

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1,8-Diazabicyclo(5.4.0)undec-7-eneHCID 81184—
Reactant1-Ethyl-6,7,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acidHCID 9835179—
Reactant2-(Formylaminomethyl)morpholine hydrochlorideHCID 19834980—
SolventAcetonitrileHCID 6342—
Product1-Ethyl-6,8-difluoro-7-[2-(formylaminomethyl)morpholino]-1,4-dihydro-4-oxoquinoline-3-carboxylic acidHCID 14652602—

Reaction Steps

A solution of 813 mg of 1-ethyl-6,7,8-trifluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid, 650 mg of 2-(formylaminomethyl)morpholine hydrochloride and 1.0 g of 1,8-diazabicyclo[5.4.0]undec-7-ene in 10 ml of acetonitrile is refluxed for 3 hours and allowed to stand at room temperature overnight. The precipitated crystals are collected by filtration and successively washed with acetonitrile, water and acetone to give 1-ethyl-6,8-difluoro-7-[2-(formylaminomethyl)morpholino]-1,4-dihydro-4-oxoquinoline-3-carboxylic acid, melting at 234°-236° C.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS04889857
Source datasetuspto-grants-1989_12
ORD IDord-86916008a3a74584aa92e85bdd727e74
Source noteuspto-grants-1989_12