Hansjoerg Lehmann, Thomas Ruppen, Susanne Oswald, Ning Ye, Xiangguang Tian, Xingxian Gu, Chunhui Dai, Robin A. Fairhurst
{"title":"Development of a Safe and Efficient Continuous Flow Method for the Synthesis of 3-Difluoromethoxypyridine Derivatives","authors":"Hansjoerg Lehmann, Thomas Ruppen, Susanne Oswald, Ning Ye, Xiangguang Tian, Xingxian Gu, Chunhui Dai, Robin A. Fairhurst","doi":"10.1002/hlca.202400182","DOIUrl":null,"url":null,"abstract":"<p>The development of a safe, efficient and scalable continuous-flow-chemistry protocol for the O-difluoromethylation of two 3-hydroxypyridine building blocks is described. This example highlights that continuous flow chemistry has become firmly established within Novartis Biomedical Research, and when implemented appropriately can enable the continuous supply of material from the first realization of a potentially interesting intermediate within a discovery project all the way through to clinical evaluation.</p>","PeriodicalId":12842,"journal":{"name":"Helvetica Chimica Acta","volume":"108 2","pages":""},"PeriodicalIF":1.5000,"publicationDate":"2024-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Helvetica Chimica Acta","FirstCategoryId":"92","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/hlca.202400182","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Development of a Safe and Efficient Continuous Flow Method for the Synthesis of 3-Difluoromethoxypyridine Derivatives
The development of a safe, efficient and scalable continuous-flow-chemistry protocol for the O-difluoromethylation of two 3-hydroxypyridine building blocks is described. This example highlights that continuous flow chemistry has become firmly established within Novartis Biomedical Research, and when implemented appropriately can enable the continuous supply of material from the first realization of a potentially interesting intermediate within a discovery project all the way through to clinical evaluation.
期刊介绍:
Helvetica Chimica Acta, founded by the Swiss Chemical Society in 1917, is a monthly multidisciplinary journal dedicated to the dissemination of knowledge in all disciplines of chemistry (organic, inorganic, physical, technical, theoretical and analytical chemistry) as well as research at the interface with other sciences, where molecular aspects are key to the findings. Helvetica Chimica Acta is committed to the publication of original, high quality papers at the frontier of scientific research. All contributions will be peer reviewed with the highest possible standards and published within 3 months of receipt, with no restriction on the length of the papers and in full color.