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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

A Flow Chemistry Approach to Norcantharidin Analogues

Author(s): Mark Tarleton, Kelly A. Young, Elli Unicomb, Siobhann N. McCluskey, Mark J. Robertson, Christopher P. Gordon and Adam McCluskey

Volume 8, Issue 6, 2011

Page: [568 - 574] Pages: 7

DOI: 10.2174/157018011795906730

Price: $65


Acid-ester and acid-amide norcantharidin derivatives are prepared using a ‘one-pot’ synthetic procedure utilizing the ThalesNano H-cube™ flow hydrogenator. Traditionally, rapid library generation and reaction scale up of these analogues was limited by the batch wise hydrogenation of 5,6-dehydronorcantharidin. This was resolved with the use of flow chemistry. With no associated scale up issues, a method was devised to produce norcantharidin, along with acid-ester and acid-amide analogues on any scale necessary for biological screening.

Keywords: Cantharidin, Norcantharidin, Flow hydrogenation, Flow chemistry, Protein phosphatase inhibition, anti-malarial, anti-parasitic, Diels, , Alder, Parr hydrogenation, H-cube, Kinomics, acetone, acid ester, nucleophilicity

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