Carvedilol → Carvedilol

HRID 47917Notes

Reaction equation

HRID 47917 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>O1CCOCC1.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][NH2:12].[CH3:1][O:2][C:3]1[CH:4]=[CH:5][CH:6]=[CH:7][C:8]=1[O:9][CH2:10][CH2:11][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:30]1[CH2:13][CH:14]1[CH2:15][O:16][C:17]1[C:22]2[C:23]3[C:28](=[CH:27][CH:26]=[CH:25][CH:24]=3)[NH:29][C:21]=2[CH:20]=[CH:19][CH:18]=1

Participants

5

Reactant 1

HCID 2585Carvedilol

Product 3

HCID 2585CarvedilolHCID 17130052-(2-Methoxyphenoxy)ethyl amineHCID 50207104-Oxiranylmethoxy-9H-carbazole

Reagents, catalysts & solvents 1

HCID 218864351,4-Dioxane--water (1/1)Solvent

Conditions

Temperature
55 °C

Procedure

Carvedilol (4 g) was dissolved in 267 mL dioxane/water in the ratio 1:1.4 respectively by heating the mixture under stirring at 55° C. water bath. The resulting solution was left at room temperature without stirring for about 15 h then the crystals were filtered through a buchner funnel and dried in a desiccator (connected to air pump) until constant weight to yield Carvedilol Form III in a mixture with Carvedilol Form II.

Workup

  1. temperatureby heating the mixture
  2. waitThe resulting solution was left at room temperature
  3. stirringwithout stirring for about 15 h
  4. filtrationthe crystals were filtered through a buchner funnel
  5. customdried in a desiccator (connected to air pump) until constant weight

Sources & evidence

ORD record
ord-64493faf84f3485f91f7ee7b65141eee
Source dataset
uspto-grants-2004_03
Patent number
US06699997B2

Reaction notes

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