Reaction equation
[N:1]1([C:10]([C:12]2[CH:17]=[CH:16][C:15]([NH:18][C:19]3[S:23][N:22]=[C:21]([OH:24])[C:20]=3[C:25]#[N:26])=[CH:14][CH:13]=2)=[O:11])[C:9]2[C:4](=[CH:5][CH:6]=[CH:7][CH:8]=2)[CH2:3][CH2:2]1.[NH2:27][CH:28]([CH3:31])[CH2:29][OH:30]>CCO>[N:1]1([C:10]([C:12]2[CH:13]=[CH:14][C:15]([NH:18][C:19]3[S:23][N:22]=[C:21]([OH:24])[C:20]=3[C:25]([NH:27][CH:28]([CH3:31])[CH2:29][OH:30])=[NH:26])=[CH:16][CH:17]=2)=[O:11])[C:9]2[C:4](=[CH:5][CH:6]=[CH:7][CH:8]=2)[CH2:3][CH2:2]1Participants
4
Reactant 2
Product 1
Reagents, catalysts & solvents 1
Conditions
- Temperature
- 80 °C
Procedure
To 5-[4-(2,3-dihydro-indole-1-carbonyl)-phenylamino]-3-hydroxy-isothiazole-4-carbonitrile 5 (0.362 gm, 1 mmol) in 10 ml anhydrous EtOH was added (2-amino-propan-1-ol (0.375 gm, 5 mmol). The reaction mixture was maintained at 80° C. for 16 h. with stirring, then concentrated to dryness and purified by column chromatography to provide 5-[4-(2,3-dihydro-indole-1-carbonyl)-phenylamino]-3-hydroxy-N-(2-hydroxy-1-methyl-ethyl)-isothiazole-4-carboxamidine 6.
Workup
- concentrationconcentrated to dryness
- custompurified by column chromatography
Sources & evidence
- ORD record
- ord-b222d67b4d094814bc0cae7ace7af241
- Source dataset
- uspto-grants-2010_01
- Patent number
- US07652047B2
Linked notes
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