Brief Introduction

The dihydroxylation of olefin is one of the most important reactions in organic synthesis and has been widely used in the field of pharmaceutical synthesis.

The dihydroxylation reaction of organic phase olefin catalyzed by quaternary ammonium salt carried out by the research team can carry out the dihydroxylation reaction of electron-deficient olefin in organic solvent at a relatively high reaction temperature (-5~5 degrees) to avoid excessive oxidation and improve the reaction yield. Good results have been obtained in the dihydroxylation reaction, a key step in the synthesis of anti-hepatitis C drug soflurbuvir. It is worth mentioning that this soflbuvir intermediate shown below is also often used in a number of other new antiviral drugs, including some new drugs against the corona-virus.

Performance indicators

Compared with the traditional method, the production rate is increased by 10% or even 20%, and it is carried out at a more reasonable reaction temperature (0-5 degrees), which is more suitable for large-scale production, saving energy and improving efficiency.

The product quality is fully up to standard, and the purity can reach more than 98% after a recrystallization.

Scope of application and market prospects

Suitable for cis-dihydroxylation of electron-deficient alkenes. For example, Soflubuvir intermediate (CAS: 93635-76-8) has been used as a key intermediate in many new antiviral drugs. Recent new drugs against the novel coronavirus contain this intermediate structural unit.

Investment estimates

For general pharmaceutical or chemical enterprises, there is basically no additional investment, and conventional reaction equipment can be used.

Means of cooperation

Technical support; technology transfer; cooperative production.