Carvedilol → Carvedilol
Reaction equation
[CH3:1][O:2][C:3]1[CH:4]=[CH:5][CH:6]=[CH:7][C:8]=1[O:9][CH2:10][CH2:11][NH:12][CH2:13][CH:14]([OH:30])[CH2:15][O:16][C:17]1[CH:18]=[CH:19][CH:20]=[C:21]2[NH:29][C:28]3[CH:27]=[CH:26][CH:25]=[CH:24][C:23]=3[C:22]=12>C(O)C.O>[CH3:1][O:2][C:3]1[CH:4]=[CH:5][CH:6]=[CH:7][C:8]=1[O:9][CH2:10][CH2:11][NH:12][CH2:13][CH:14]([OH:30])[CH2:15][O:16][C:17]1[CH:18]=[CH:19][CH:20]=[C:21]2[NH:29][C:28]3[CH:27]=[CH:26][CH:25]=[CH:24][C:23]=3[C:22]=12.[CH3:1][O:2][C:3]1[CH:4]=[CH:5][CH:6]=[CH:7][C:8]=1[O:9][CH2:10][CH2:11][NH2:12]Participants
5
Reactant 1
Product 2
Reagents, catalysts & solvents 2
Conditions
- Temperature
- 55 °C
Procedure
Carvedilol (4 g) was dissolved in 45 mL of a mixture of 96% Ethanol and 4% water by heating the mixture under stirring in a 55° C. water bath. The solution was cooled and left at room temperature without stirring for about 14 hours, the crystals were filtered through a buchner funnel, rinsed twice with about 10 ml cold (4° C.) 96% ethanol, and dried in a desiccator at room temperature (connected to air pump) until constant weight to yield carvedilol Form III.
Workup
- temperatureby heating the mixture
- temperatureThe solution was cooled
- waitleft at room temperature
- stirringwithout stirring for about 14 hours
- filtrationthe crystals were filtered through a buchner funnel
- washrinsed twice with about 10 ml cold (4° C.) 96% ethanol
- customdried in a desiccator at room temperature (connected to air pump) until constant weight
Sources & evidence
- ORD record
- ord-3bcd68efaf7840a3b34d9febee822c9c
- Source dataset
- uspto-grants-2004_03
- Patent number
- US06699997B2
Reaction notes
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