Development of Process Synthesis Method of NEt-3IB–Aiming to reduce the waste in API synthesis–

 We succeeded in developing a large-scale synthetic method of NEt-3IB which is expected to contribute to SDGs by reducing the volume of waste liquid. Inflammatory bowel disease (IBD) is a disease associated with diarrhea, bloody stools, and abdominal pain due to chronic inflammation for which the number of patients is increasing worldwide. Steroids and antibody drugs have been marketed as therapeutic agents, However, they could not induce mucosal healing. NEt-3IB, which we have developed, has been developing as an anti-IBD small-drug candidate which enables to reduce inflammation and induce mucosal healing.

✔️ Converting the organic solvent used into a hydrophobic ether, which can be recovered and reused,enabled to reduce the number of solvent species and volume of waste liquid.
✔️ Avoiding complicated purification such as column chromatography and improving the overall yield.
✔️ Succeeded in significantly improving the E-factor, which is an index of environmentally synthetic method,compared to the conventional method.
✔️ Expected to contribute to “Healthy and Wellbeing for All (SDG 3)” and “Safe Water and Toilets worldwide (SDG 6)” through the development of small-molecule IBD drug and reduction of waste in API synthesis.


 

(Kakuta H et. al. Chem. Pharm. Bull., 2021, 70, 146–154.)

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