Carvedilol → Carvedilol

HRID 1723893Notes

Reaction equation

HRID 1723893 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-8f6b426428cd41589c6e0b0dc67f5a2d
Source dataset
uspto-grants-2009_02
Patent number
US07485663B2

Reaction notes

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