Gagan Kukreja’s Post

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Associate Director, Medicinal Chemistry, SynVent IDD, Syngene

There has always been a dearth of practical and efficient methods for accessing organic nitrates, which are quite famous in the pharmaceutical industry as effective donors of the signaling molecule nitric oxide, exemplified by well-known drugs such as glycerol trinitrate and isosorbide mononitrate. A new study reports practical and regioselective halonitrooxylation of a wide variety of unactivated olefins to access β-halonitrates. The protocol offers high efficiency, mild conditions, simple operation, and good compatibility with various functional groups. Especially, the product of ethylene iodonitrooxylation, 2-iodoethyl nitrate, can be combined with a range of natural products and drugs to obtain corresponding nitrooxylated functional molecules. The potential utility of the method is further highlighted by the gram-scale preparation and late-stage modification of bioactive molecules. https://lnkd.in/gYPNw-fj

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