Trifluoroacetic acid → HCID 59519024, compound
Reaction equation
C(OC([N:8]1[CH2:11][CH:10]([CH2:12][N:13]2[CH2:18][CH2:17][CH2:16][CH2:15][CH2:14]2)[CH2:9]1)=O)(C)(C)C.C(O)(C(F)(F)F)=O.C(Cl)Cl.FC(F)(F)C(O)=O>>[NH:8]1[CH2:9][CH:10]([CH2:12][N:13]2[CH2:14][CH2:15][CH2:16][CH2:17][CH2:18]2)[CH2:11]1Participants
4
Procedure
3-Piperidin-1-ylmethylazetidine-1-carboxylic acid tert-butyl ester (180 mg, 0.70 mmol) was treated with a solution of TFA:DCM (1:1 v/v, 5 mL) and the resultant solution stirred at room temperature for 1 h. The solution was concentrated in vacuo afford 1-azetidin-3-ylmethylpiperidine (INTERMEDIATE III.1) (190 mg, 0.70 mmol, 100%) as the trifluoroacetic acid salt which was used without further purification.
Workup
- concentrationThe solution was concentrated in vacuo
Sources & evidence
- ORD record
- ord-7d5249f8b5b944e58f3974daf4cddf5f
- Source dataset
- uspto-grants-2010_10
- Patent number
- US07820649B2
Reaction notes
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