Trifluoroacetic acid methylene chloride → 3-Methoxyazetidine 2,2,2-trifluoroacetate
Reaction equation
[CH3:1][O:2][CH:3]1[CH2:6][N:5](C(OC(C)(C)C)=O)[CH2:4]1.[C:14]([OH:20])([C:16]([F:19])([F:18])[F:17])=[O:15].C(Cl)Cl>>[F:17][C:16]([F:19])([F:18])[C:14]([OH:20])=[O:15].[CH3:1][O:2][CH:3]1[CH2:6][NH:5][CH2:4]1Participants
3
Procedure
A solution of tert-butyl 3-methoxyazetidine-1-carboxylate (270 mg, 1.44 mmol) in 1:1 TFA/DCM (1 mL) was stirred at ambient temperature for 1 hour and concentrated. The crude product was directly used in the next step assuming quantitative yield.
Workup
- concentrationconcentrated
Sources & evidence
- ORD record
- ord-5631f0ad3b744cc18f519abfe3b71890
- Source dataset
- uspto-grants-2014_07
- Patent number
- US08791123B2
Reaction notes
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