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Phosphorylation

Phosphorylation is a chemical process that usually refers to the esterification reaction between hydroxy compounds (such as fatty alcohols, alkyl phenols, lipids, etc.) and phosphorylation reagents. The developed phosphate esters can be classified as phosphomonoester, phosphodiesters and phosphotriesters. It has been demonstrated that the introduction of phosphate groups into the molecular structure of an organic compound can not only significantly improve the physicochemical properties of the chemical substance such as solubleness and stability, but also enhance the pharmacological activities such as safety and potency. Therefore, phosphorylation has become one of the most concerned research areas in many fields including food industry, cosmetics, and especially the pharmaceuticals.

Below is a list of our Synthetic Routes for Phosphate Esters (include but not limited to the following):

  • Synthetic method based on phosphorus pentoxide and alcohol

Phosphorus pentoxide has the advantages with simplicity and feasibility, mild conditions, simple equipment, high yield, and low cost. Since the product of this reaction is a mixture of mono- and di-esters and the composition is indefinite, this reaction is not suitable for the synthesis of phosphate ester as an intermediate.

  • Synthetic method based on phosphoric acid (or polyphosphoric acid) and alcohol

The method is characterized by high stability of phosphoric acid (or polyphosphoric acid) as raw materials, convenient metering of the ratio of ingredients, easy control of the process, no emission of waste gas and waste liquid, and broad prospects for industrial applications.

  • Synthetic method based on phosphorus trichloride and alcohol

In this method, an appropriate amount of chlorine gas is added during the reaction and a small amount of water is added. The content of phosphodiesters in the product is relatively high, but the product contains HCl, which causes corrosion of the equipment. Our new reaction equipment is fabricated from stainless steel, which can accommodate most reagents.

In addition to the above, there are other methods for the synthesis of phosphate esters, such as the reaction of phosphoric acid (or phosphate) with halogenated hydrocarbons, the reaction of phosphoric acid with epoxy compounds, transesterification, extraction of natural products, and so on.

Why Choose BOC Sciences?

BOC Sciences is specialized in the design and production of phosphate ester functional monomers with different functions and different carbon chain structures while providing industrial solutions for the specific performance requirements such as resistance to boiling, heat resistance, moisture resistance, and corrosion resistance. We have a wealth of technical reserves and to provide customers with specifically customized services. BOC Sciences will ensure that the appropriate method is utilized for your specific phosphorylation process. At the same time, we also have different analytical methods including: mixed indicator method, potential or conductivity titration, 31P-NMR spectroscopy, thin layer chromatography, etc. Please contact us if you have special structural requirements or performance requirements.

Reference

  1. Ji, X., Wang, J., Zhang, L., Zhao, L. X., Jiang, H. L., & Liu, H. (2013). Application of phosphates and phosphonates prodrugs in drug research and development. Yao xue xue bao= Acta pharmaceutica Sinica48(5), 621-634.
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