Tapentadol Hydrochloride suppliers
Tapentadol Hydrochloride
- CAS:
- 175591-09-0
- MF:
- C14H24ClNO
- MW:
- 257.81
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Properties
- Melting point:
- 178-194°C
- Flash point:
- 9℃
- storage temp.
- -20°C Freezer, Under Inert Atmosphere
- solubility
- DMF: 20 mg/ml; DMSO: 25 mg/ml; Ethanol: 20 mg/ml; PBS (pH 7.2): 10 mg/ml
- form
- A neat solid
Safety Information
- Symbol(GHS)
GHS02,GHS06,GHS08
- Signal word
- Danger
- Hazard statements
- H225-H301+H311+H331-H370
- Precautionary statements
- P210-P260-P280-P301+P310-P311
- Hazard Codes
- F,T
- Risk Statements
- 11-23/24/25-39/23/24/25
- Safety Statements
- 7-16-36/37-45
- RIDADR
- UN1230 - class 3 - PG 2 - Methanol, solution
- WGK Germany
- 1
Use
The synthesis of tapentadol hydrochloride begins with diethyl ketone, which is subjected to a standard Mannich condition to provide a b-dimethylamino intermediate. A Grignard reaction with 3-bromoanisole was followed by the separation of diastereomers and racemic resolution. Treatment with thionyl chloride converts the hydroxy group to its corresponding chloride, which is removed by treatment with zinc borohydride (generated from zinc chloride and sodium borohydride), with overall retention of stereochemistry. The methyl ether is cleaved in refluxing HBr to afford the tapentadol salt that is ultimately converted to the hydrochloride for formulation into 50-, 75-, and 100-mg immediate-release (IR) oral tablets.
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