Hydrochloric Acid → Tiapride Hydrochloride

HRID 982575Notes

Reaction equation

HRID 982575 reaction equation
C(O)(=O)C(C(C(O)=O)O)O.O.[CH3:12][CH2:13][N:14]([CH2:17][CH2:18][NH:19][C:20]([C:22]1[CH:23]=[C:24]([S:30]([CH3:33])(=[O:32])=[O:31])[CH:25]=[CH:26][C:27]=1[O:28][CH3:29])=[O:21])[CH2:15][CH3:16].[ClH:34]>>[CH3:16][CH2:15][N:14]([CH2:17][CH2:18][NH:19][C:20]([C:22]1[CH:23]=[C:24]([S:30]([CH3:33])(=[O:32])=[O:31])[CH:25]=[CH:26][C:27]=1[O:28][CH3:29])=[O:21])[CH2:13][CH3:12].[ClH:34]

Participants

5

Reactant 4

HCID 313Hydrochloric AcidHCID 8752,3-Dihydroxybutanedioic AcidHCID 962WaterHCID 5467Tiapride

Product 1

HCID 5702214Tiapride Hydrochloride

Procedure

Two granules are prepared. For granule 1, Methocel® K100M, Avicel® PH102 and tartaric acid are dry-mixed and then granulated with water in a granulating blender and the granules obtained are then dried. The other components, magnesium stearate, Aerosile® 200 and monosodium carbonate are then dry-added and mixed. For granule 2, tiapride hydrochloride, Methocel® and Avicel® are dry-mixed and are then granulated with water in a granulating blender and the granules obtained are then dried. Magnesium stearate and Aerosile® are dry-added and mixed. 3-layer tablets are prepared, containing 250 mg of granule 1 in the first outer layer, 280 mg of granule 2 in the inner layer, which contains 100 mg of base tiapride in hydrochloride form, and 200 mg of granule 1 in the second outer layer.

Workup

  1. customTwo granules are prepared
  2. customthe granules obtained
  3. customare then dried
  4. additionThe other components, magnesium stearate, Aerosile® 200 and monosodium carbonate are then dry-added
  5. additionmixed
  6. additionFor granule 2, tiapride hydrochloride, Methocel® and Avicel® are dry-mixed
  7. customthe granules obtained
  8. customare then dried
  9. additionMagnesium stearate and Aerosile® are dry-added
  10. additionmixed
  11. custom3-layer tablets are prepared
  12. additioncontaining 250 mg of granule 1 in the first outer layer, 280 mg of granule 2 in the inner layer, which

Sources & evidence

ORD record
ord-6476f3cbeb6643959e1a404384a9d32c
Source dataset
uspto-grants-2005_03
Patent number
US06861072B1

Reaction notes

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