2-Chloro-3-(trifluoromethyl)pyridine → 3-Methyl-1-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Reaction equation
C[Si](C)(C)C1C=C(C=CC=1)N.Cl[C:13]1[C:18]([C:19]([F:22])([F:21])[F:20])=[CH:17][CH:16]=[CH:15][N:14]=1.[CH3:23][C@@H:24]1[CH2:29][NH:28][CH2:27][CH2:26][NH:25]1>>[CH3:23][CH:24]1[NH:25][CH2:26][CH2:27][N:28]([C:13]2[C:18]([C:19]([F:22])([F:21])[F:20])=[CH:17][CH:16]=[CH:15][N:14]=2)[CH2:29]1Participants
4
Procedure
Compound A-03 can be synthesized according to method 1. Just of Scheme 1, R1 is —CF3; R2 is -Me; R3 is p-SiMe3. More specifically, compound 1 is 2-chloro-3-(trifluoromethyl)-pyridine (2 g); compound 2 is (R)-2-methylpiperazine; the synthesized compound 3 is 3-methyl-1-(3-trifluoromethyl-2-pyridyl)piperazine (2.5 g, yield about 92.6%).
Workup
- customCompound A-03 can be synthesized
Sources & evidence
- ORD record
- ord-8a7044d1d7f24205b4d14a222192fb8b
- Source dataset
- uspto-grants-2014_06
- Patent number
- US08748610B2
Reaction notes
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