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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1788350Generated: November 4, 2026

3,5-Bis(trifluoromethyl)phenyl isocyanate → Tert-butyl 4-[1-({[3,5-bis(trifluoromethyl)phenyl]amino}carbonyl)azetidin-3-yl]piperazine-1-carboxylate

https://huagongshe.com/reaction/1788350

Reaction equation

Participants

RoleNameHCIDCharge
Reactant3,5-Bis(trifluoromethyl)phenyl isocyanateHCID 2733314—
Reactanttert-Butyl 4-(azetidin-3-yl)piperazine-1-carboxylateHCID 21183794—
SolventTetrahydrofuranHCID 8028—
ProductTert-butyl 4-[1-({[3,5-bis(trifluoromethyl)phenyl]amino}carbonyl)azetidin-3-yl]piperazine-1-carboxylateHCID 23140263—

Reaction Steps

To a solution of the compound prepared in Example 2 (986 mg) in tetrahydrofuran (12 mL) was dropwise added 1-isocyanato-3,5-bis(trifluoromethyl)benzene (0.85 mL), and the mixture was stirred for 30 minutes. The reaction solution was concentrated. The residue was purified by column chromatography on silica gel (hexane:ethyl acetate=1:1) to give the compound of the present invention (1.413 g) having the following physical data.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07511159B2
Source datasetuspto-grants-2009_03
ORD IDord-4559a6888c6b47bd998d55458b50c4ed
Source noteuspto-grants-2009_03