3,5-Bis(trifluoromethyl)phenyl isocyanate → Tert-butyl 4-[1-({[3,5-bis(trifluoromethyl)phenyl]amino}carbonyl)azetidin-3-yl]piperazine-1-carboxylate
Reaction equation
[NH:1]1[CH2:4][CH:3]([N:5]2[CH2:10][CH2:9][N:8]([C:11]([O:13][C:14]([CH3:17])([CH3:16])[CH3:15])=[O:12])[CH2:7][CH2:6]2)[CH2:2]1.[N:18]([C:21]1[CH:26]=[C:25]([C:27]([F:30])([F:29])[F:28])[CH:24]=[C:23]([C:31]([F:34])([F:33])[F:32])[CH:22]=1)=[C:19]=[O:20]>O1CCCC1>[F:28][C:27]([F:29])([F:30])[C:25]1[CH:26]=[C:21]([NH:18][C:19]([N:1]2[CH2:4][CH:3]([N:5]3[CH2:10][CH2:9][N:8]([C:11]([O:13][C:14]([CH3:17])([CH3:16])[CH3:15])=[O:12])[CH2:7][CH2:6]3)[CH2:2]2)=[O:20])[CH:22]=[C:23]([C:31]([F:34])([F:32])[F:33])[CH:24]=1Participants
4
Reactant 2
Product 1
Reagents, catalysts & solvents 1
Procedure
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.