There is no cure for inflammatory bowel disease (IBD) but scientists from Japan may have uncovered a new technique that could help in creating an effective and sustainable drug. For creating a small-molecule drug, researchers developed a large-scale synthesis method for easily developing a compound necessary for IBD treatment.
“We have successfully developed new method for mass-synthesizing environmentally friendly NEt-3IB with a 35-fold better E-factor—an indicator of the environmental burden in multistage drug substance synthesis—than conventional processes,” says Dr. Hiroki Kakuta, an associate professor at Okayama University, in a statement.
NEt-3IB stands for 4-(ethyl(3-isobutoxy-4-isopropylphenyl)amino)benzoic acid which is in high demand in developing treatments for IBD. The new method promises to create a more widespread and stable supply of this compound, allowing researchers to design small-molecule drugs that are both cost-effective and easy to administer.
The motivation behind this method comes from the need to optimize normal processes for NEt-31B synthesis. “The synthesis of NEt-3IB so conventionally uses column chromatography, which requires a large amount of organic solvents in addition to three organic solvents that are not recoverable for reaction. In order to achieve carbon neutrality and meet sustainable development goals (SDGs), we were driven to avoid column chromatography and find approaches with recoverable organic solvents,” explains Dr. Kakuta.
The new process uses only fat-soluble ether and alcohol. Doing so will cause a substantial decrease in the volume of liquid waste and allow for easy recycling. Purifying the NEt-3IB through recrystallization verified the method’s effectiveness with a total yield of over 30% and a purity of 99%.
“Our method provides an example of an approach that employs recoverable solvents and takes a step towards carbon neutrality. This approach can be applied for the production of not only NEt-3IB, but also other small molecule pharmaceuticals,” adds Dr. Kakuta.
The study is published in the Chemical and Pharmaceutical Bulletin.