(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-methylphenol 2,3-dihydroxysuccinate → Tolterodine

HRID 237179

Reaction equation

HRID 237179 reaction equation
[CH3:1][C:2]1[CH:3]=[CH:4][C:5]([OH:24])=[C:6]([C@@H:8]([C:18]2[CH:19]=[CH:20][CH:21]=[CH:22][CH:23]=2)[CH2:9][CH2:10][N:11]([CH:15]([CH3:17])[CH3:16])[CH:12]([CH3:14])[CH3:13])[CH:7]=1.C(O)(C(O)=O)C(O)C(O)=O>O>[CH3:1][C:2]1[CH:3]=[CH:4][C:5]([OH:24])=[C:6]([C@@H:8]([C:18]2[CH:19]=[CH:20][CH:21]=[CH:22][CH:23]=2)[CH2:9][CH2:10][N:11]([CH:12]([CH3:14])[CH3:13])[CH:15]([CH3:16])[CH3:17])[CH:7]=1

Participants

3

Reactant 1

HCID 9847786(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-methylphenol 2,3-dihydroxysuccinate

Product 1

HCID 443879Tolterodine

Reagents, catalysts & solvents 1

HCID 962WaterSolvent

Procedure

Tolterodine tartrate, microcrystalline cellulose and part of ethylcellulose are blended with small amount of water into homogeneous blend from which pellet cores are made by extrusion and spheronization. Dry pellet cores are coated with the coating dispersion of Example 8. Within first hour almost 50% dissolves, however between 7 and 16 hours less dissolves as compared to Example 2.

Workup

  1. customDry pellet cores
  2. dissolutionWithin first hour almost 50% dissolves, however between 7 and 16 hours
  3. dissolutionless dissolves

Sources & evidence

ORD record
ord-cc18d6845501455995a9f42bb0d6eea0
Source dataset
uspto-grants-2014_02
Patent number
US08642078B2

Linked notes

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