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• W2909969662 abstract "An efficient synthesis of pyridopyrazine-1,6-dione γ-secretase modulators (GSMs) is described. Our route features the construction of a crystalline lactone intermediate via a selective palladium-catalyzed 4-methylimidazole N1-arylation using the Buchwald Xantphos Pd G4 precatalyst, which does not require a preactivation step. The weak inorganic base KHCO3 was employed to minimize saponification of a particularly sensitive lactone substrate. Additional key transformations include DABAL-Me3-mediated lactone aminolysis and a mild TBD/ethyl trifluoroacetate mediated lactam ring closure to afford a representative GSM in high yield." @default.
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• W2909969662 date "2019-01-08" @default.
• W2909969662 modified "2023-09-27" @default.
• W2909969662 title "Synthesis of Pyridopyrazine-1,6-dione γ-Secretase Modulators via Selective 4-Methylimidazole <i>N</i>¹-Buchwald Arylation" @default.
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• W2909969662 doi "https://doi.org/10.1021/acs.joc.8b02953" @default.
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