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The Production Process of N-Methyl-N-(phenylmethyl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-pyridinamine: A Comprehensive Review
Meta Title: The Production Process of N-Methyl-N-(phenylmethyl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-pyridinamine: A Comprehensive Review
Meta Description: This article provides a comprehensive review of the production process of N-Methyl-N-(phenylmethyl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-pyridinamine, which is a widely used intermediate in the pharmaceutical industry.
Introduction:
N-Methyl-N-(phenylmethyl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2-pyridinamine, commonly referred to as DMF-BORON, is a key intermediate used in the production of various drugs, including HIV protease inhibitors.
The synthesis of DMF-BORON involves several steps, which require careful optimization to ensure high yield and purity.
This article provides a comprehensive review of the production process of DMF-BORON, covering the synthesis of its starting materials, the synthesis of DMF-BORON itself, and the purification and isolation of the final product.
Synthesis of Starting Materials:
The synthesis of DMF-BORON starts with the synthesis of its starting materials, including (S)-2-((2-((2-nitro-4-trifluoromethylphenyl)amino)-5-methyl-4,4-dimethyl-oxazepin-7-yl)amino)-N-(2,6-dimethylphenyl)acetamide (Compound 1) and N-(2-((3S)-3-(difluoromethyl)-1,3-oxazolidin-2-yl)-5-methyl-4,4-dimethyl-oxazepin-7-yl)acetamide (Compound 2).
These starting materials are synthesized through a series of reactions involving the nucleophilic substitution of a halogen atom with a reactive center, such as an amino or hydroxyl group.
The synthesis of these compounds requires careful selection of reagents and conditions to ensure high yield and purity.
Synthesis of DMF-BORON:
Once the starting materials are synthesized, the next step is the synthesis of DMF-BORON itself.
DMF-BORON is synthesized through a series of reactions involving the reaction of Compound 1 and Compound 2 with boron cluster compounds, such as borabenzene dicarboxylate (BDBC), in the presence of a catalyst, such as lithium dimethylformamide.
The reaction involves the formation of a boron-carbon bond, followed by the elimination of trimethylphosphine to form the final product.
The synthesis of DMF-BORON requires careful optimization of the reaction conditions, including the concentration of the reactants, the presence of a catalyst, and the solvent used.
Purification and Isolation of DMF-BORON:
The final step in the production process of DMF-BORON is the purification and isolation of the final product.
This step involves the removal of impurities, such as solvent, unreacted starting materials, and other by-products, to produce a pure sample of DMF-BORON