Carvedilol → Carvedilol

HRID 47914Notes

Reaction equation

HRID 47914 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>O.CO>[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

4

Reactant 1

HCID 2585Carvedilol

Product 2

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

Reagents, catalysts & solvents 1

HCID 22242641Methanol--water (1/1)Solvent

Conditions

Temperature
55 °C

Procedure

Carvedilol (4 g) was dissolved in 195 mL mixture of water/methanol (in a ratio 1:3 respectively) by heating the mixture under stirring in 55° C. water bath. The solution cooled to ambient temperature and left at ambient temperature without stirring for about 15 h, the crystals were filtered through a buchner 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 cooled to ambient temperature
  3. waitleft at ambient temperature
  4. stirringwithout stirring for about 15 h
  5. filtrationthe crystals were filtered through a buchner
  6. customdried in a desiccator at room temperature (connected to air pump) until constant weight

Sources & evidence

ORD record
ord-6a41a9615c514b78a4a3ff9d034e5297
Source dataset
uspto-grants-2004_03
Patent number
US06699997B2

Reaction notes

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