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- ISSN: 1570-1808
- E-ISSN: 1875-628X
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A Flow Chemistry Approach to Norcantharidin Analogues
- Source: Letters in Drug Design & Discovery, Volume 8, Issue 6, Jul 2011, p. 568 - 574
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- 01 Jul 2011
Abstract
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.
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