Ethanol → 5-(Propan-2-yl)-1,3-thiazol-2-amine
Reaction equation
[CH3:1][CH:2]([CH3:6])[CH2:3][CH:4]=O.BrBr.[NH2:9][C:10]([NH2:12])=[S:11].C(O)C>O1CCOCC1>[NH2:12][C:10]1[S:11][C:3]([CH:2]([CH3:6])[CH3:1])=[CH:4][N:9]=1Participants
Reactant 4
Product 1
Reagents, catalysts & solvents 1
Procedure
2 ml (18.6 mmol) of 3-methylbutyraldehyde were dissolved in 15 ml of dioxane. 40.4 ml (18.6 mmol) of a solution 2% v/v of bromine in dioxane was dropped therein at 0° C. The mixture was maintained at room temperature under stirring for 2 hours, then 2.83 g (37.2 mmol) of thiourea and 5 ml of ethanol were added. After 6 hours at room temperature the solution was evaporated to dryness, the residue was dissolved in methylene chloride and the product extracted with 1M hydrochloric acid; the aqueous layer was made basic by using 30% ammonium hydrate and extracted again with methylene chloride. The organic phase was dried over sodium sulfate and evaporated under vacuum. The residue was chromatographed on a silica gel column, eluting with cyclohexane-ethylacetate to give 1.1 g (42% yield) of the title compound.
Workup
- customat 0° C
- customAfter 6 hours at room temperature the solution was evaporated to dryness
- dissolutionthe residue was dissolved in methylene chloride
- extractionthe product extracted with 1M hydrochloric acid
- extractionextracted again with methylene chloride
- dry with materialThe organic phase was dried over sodium sulfate
- customevaporated under vacuum
- customThe residue was chromatographed on a silica gel column
- washeluting with cyclohexane-ethylacetate
Sources & evidence
- ORD record
- ord-3ea8831d7c244e2dbc45853cf813d07c
- Source dataset
- uspto-grants-2006_05
- Patent number
- US07037929B1
Reaction notes
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