Carvedilol → Carvedilol

HRID 1828011Notes

Reaction equation

HRID 1828011 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

HCID 2585Carvedilol

Product 2

HCID 2585CarvedilolHCID 17130052-(2-Methoxyphenoxy)ethyl amine

Reagents, catalysts & solvents 2

HCID 702EthanolSolventHCID 962WaterSolvent

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

  1. temperatureby heating the mixture
  2. temperatureThe solution was cooled
  3. waitleft at room temperature
  4. stirringwithout stirring for about 14 hours
  5. filtrationthe crystals were filtered through a buchner funnel
  6. washrinsed twice with about 10 ml cold (4° C.) 96% ethanol
  7. customdried in a desiccator at room temperature (connected to air pump) until constant weight

Sources & evidence

ORD record
ord-16f36fd81b93402fbdd6834246d4b3d0
Source dataset
uspto-grants-2006_06
Patent number
US07056942B2

Reaction notes

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