Iodine → 5-tert-butyl-3-(3-methylbut-2-enyl)thiazol-2(3H)-imine
Reaction equation
[CH3:1][C:2]([CH3:7])([CH3:6])[CH2:3][CH:4]=O.Cl.[CH3:9][C:10]([CH3:14])=[CH:11][CH2:12][NH2:13].C(N(CC)CC)C.[C:22]([S-:24])#[N:23].[K+].II>CC#N>[C:2]([C:3]1[S:24][C:22](=[NH:23])[N:13]([CH2:12][CH:11]=[C:10]([CH3:14])[CH3:9])[CH:4]=1)([CH3:7])([CH3:6])[CH3:1]Participants
7
Procedure
3,3-Dimethylbutanal (0.95 g, 9.1 mmol), 3-methylbut-2-enyl-amine hydrochloride (1.1 g, 9.1 mmol), and triethylamine (1.3 mL, 9.1 mmol) were mixed in 9 mL of dry MeCN with 2 g of 4 Å (8-12 mesh beads) molecular sieves and stirred for 20 hours at room temperature. The reaction was filtered through Celite and washed with 8 mL of MeCN. KSCN (1.2 g, 12.3 mmol) was added and the mixture warmed to 50° C. Iodine (2.3 g, 9.1 mmol) was added and the reaction stirred at 50° C. for 6 hours. 20% Na2S2O5 was added, stirred for 30 minutes and the organic layer separated, dried with Na2SO4 and the solvent removed. The resulting solid was used without further purification. LC/MS m/z 225.3 (M+H)+.
Workup
- filtrationThe reaction was filtered through Celite
- washwashed with 8 mL of MeCN
- temperaturethe mixture warmed to 50° C
- stirringthe reaction stirred at 50° C. for 6 hours
- stirringstirred for 30 minutes
- customthe organic layer separated
- dry with materialdried with Na2SO4
- customthe solvent removed
- customThe resulting solid was used without further purification
Sources & evidence
- ORD record
- ord-7a5c4554b89e4ff297486e9ea118ba27
- Source dataset
- uspto-grants-2011_01
- Patent number
- US07875640B2
Reaction notes
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