Continuous flow hydrogenation of trans-4,5-diamino cyclopentenones to diamino cyclopentanones and base-promoted elimination originates α-enaminones. The strategy is applied to the short synthesis of reported ATP-sensitive potassium channel agonist.
Monosubstituted aniline derivatives of (7-deaza)purines have been efficiently synthesized through reductive amination of diversely functionalized aldehydes, including N-Boc protected derivatives.
Two new series of arylpurines mimicking sinefungin have been synthesized and evaluated as ZIKV methyltransferase inhibitors.
Development of a telescopic sequence for the last two steps in the CPL302415 synthesis (71.6% total yield). The procedure was generalized into the synthesis of other biologically active PI3Kδ inhibitors based on the pyrazolo[1,5-a]pyrimidine core.
Graphical abstract image generated with Copilot.