Microsoft powerpoint - sulhpoxide_microreactor_production.ppt [compatibility mode]

NCL Innovations: Solutions from CSIR India Sulphoxide compounds such as modafinil/prazole compounds are currently produced by batch synthesis procedure  The process yields about 85% product over a duration of 1-4 hours under low temperatures- leading to long processing times A more efficient process is required at the industrial level  These compounds are mainly used as proton pump inhibitors  Which consumes less time and yields lower unnecessary side products continually unlike the Our process is a continuous flow synthesis of sulphoxide compounds with reaction times of ≤ 1 minute  The reaction results in over 90% conversion and over 95% selectivity towards the target sulphoxide compounds (with less than 5% formation of undesired sulphone compounds) The process can be used to make the following drugs which are mainly used as proton pump inhibitors- used to make drugs to treat the acid-related diseases of the gastrointestinal (GI) tract  Such as omeprazole, pantoprazole, lansoprazole, tenatoprazole, rabeprazole, The process can also be used to make drug molecules that can be used as modafinil compounds  Which can be used as central nervous system stimulants- wakefulness promoting agents*  In production of drugs which act as neuroprotective agents * http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4236 GI disorders have been projected to affect more than a 250 million people in the 7 large pharma markets by 20121  Overall GI tract disorders treatment market is expected to reach $32.2 billion by 20142 In 2009, proton pump inhibitors were the third largest ther amounting up to $13.6 billion of sales in the US3 http://www.astrazeneca-annualreports.com/documents/2010/therapy_review_area_factsheets/gastrointestinal.pdfhttp://www.prnewswire.com/news-releases/reportlinker-adds-gastrointestinal-pharmaceuticals-technologies-and-markets-68849697.html 2http://www.imshealth.com/portal/site/imshealth/menuitem.a46c6d4df3db4b3d88f611019418c22a/?vgnextoid=d690a27e9d5b7210VgnVCM100000ed152ca2RCRD3  The process is continuous with the reaction time of ≤ 1 minute Results in high yield of the product with 95% of selectivity towards the sulphoxide compounds  Side product (sulphone compounds) formation- less than 5% volatile solvent that evaporates at room temperature and changes the reaction mass)  WO/ PCT application: PCT/IN2010/000456 ) )Micromixer as a Continuous Flow Reactor for the Synthesis of a Pharmaceutical Intermediate, Korean J. Chem. Eng., 20(2), 268-272 Contact Info:
Dr. Magesh N.
Scientist, NCL Innovations
National Chemical Laboratory
Pune - 411008
Phone: +91-20-2590-2982
F
Email: m(dot)nandagopal(at)ncl(dot)res(dot)in Technology Summary
Continuous flow synthesis of sulphoxide compounds for use in drug fo Technology readiness level Demonstrated at lab levelLicensing status

Source: http://www.nclinnovations.org/pdfs/available_knowhow/Sulhpoxide_Microreactor_production.pdf

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