1,1,1-Trifluoro-2-iodoethane → 5-fluoro-3-iodo-1-(2,2,2-trifluoroethyl)-1H-indazole
Reaction equation
[F:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[NH:7][N:6]=[C:5]2[I:11].[F:12][C:13]([F:17])([F:16])[CH2:14]I>>[F:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[N:7]([CH2:14][C:13]([F:17])([F:16])[F:12])[N:6]=[C:5]2[I:11]Participants
3
Procedure
The title compound was prepared in 46% yield from 5-fluoro-3-iodo-indazole and 1,1,1-trifluoro-2-iodoethane according to the general procedure for Preparation 10A. The minor isomer was not isolated or characterized. 1H NMR (400 MHz, CDCl3): δ 4.91-4.97 (2H, m), 7.17 (1H, dd, J=2.0, 8.0 Hz), 7.30 (1H, td, J=2.0, 8.4 Hz), 7.38 (1H, dd, J=3.6, 9.2 Hz).
Workup
- customThe minor isomer was not isolated
Sources & evidence
- ORD record
- ord-35de4aaa0df340adb0fd0d1b61db280d
- Source dataset
- uspto-grants-2015_03
- Patent number
- US08969343B2
Reaction notes
Loading…