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The production process of (2S,3R)-2-[(1R)-1-(3,5-bis-trifluoro-methylphenyl)ethoxy]-3-(4-fluorophenyl)morpholine involves several steps, each of which requires careful planning and execution to ensure the desired product is produced in high yield and purity.
The production process can be broken down into the following steps:
- Synthesis of 1-(3,5-bis-trifluoro-methylphenyl)ethanone
The first step in the production process is the synthesis of 1-(3,5-bis-trifluoro-methylphenyl)ethanone.
This compound is synthesized by reacting 3,5-bis-trifluoro-methylphenylamine with ethyl bromide in the presence of a base, such as sodium hydroxide.
The reaction is then followed by precipitation of the product with water. - Protection of the hydroxy group
The next step is to protect the hydroxy group of 1-(3,5-bis-trifluoro-methylphenyl)ethanone.
This is typically done by treating the compound with a protecting group, such as tert-butyldimethylsilyl chloride.
This reaction is followed by quenching of the excess reagent with sodium carbonate. - Nucleophilic substitution
The protected 1-(3,5-bis-trifluoro-methylphenyl)ethanone is then treated with a suitable nucleophile, such as dimethyl sulfate.
This reaction results in the formation of the desired compound, which is then extracted with a suitable solvent, such as ethyl acetate. - Deprotection
The next step is to deprotect the compound by treating it with a suitable reagent, such as tetrabutylammonium fluoride.
This reaction results in the formation of the desired product, which is then purified by chromatography. - Synthesis of (2S,3R)-2-[(1R)-1-(3,5-bis-trifluoro-methylphenyl)ethoxy]-3-(4-fluorophenyl)morpholine
The final step in the production process is the synthesis of (2S,3R)-2-[(1R)-1-(3,5-bis-trifluoro-methylphenyl)ethoxy]-3-(4-fluorophenyl)morpholine.
This is typically done by reacting the protected compound from step 3 with a suitable reagent, such as (2S,3R)-2-(4-fluorophenyl)-N-[(1R)-1-(3,5-bis-trifluoro-methylphenyl)ethoxy]acetamide.
The reaction is then followed by purification of the product by chromatography.
In conclusion, the production process of (2S,3R)-2-[(1R)-1-(3,5-bis-trifluoro-methylphenyl)ethoxy]-3-(4-fluorophenyl)morpholine requires careful planning and execution, with each step requiring specialized equipment and conditions.
The purification and isolation of the final product is critical for ensuring its quality and purity.
The availability of high-quality reagents and the expertise of the synthetic organic chemist are also crucial for the success of this process.