Here
we develop a novel visible-light-driven three-component cyclization
by trapping an 1,3-vinylimine ion intermediate for the direct synthesis
of pyrimido[1,2-b]indazole derivatives from bromodifluoroacetic
acid derivatives, enaminones, and 3-aminoindazoles under mild conditions.
Notably, the robust methodology provides a valuable opportunity for
the introduction of aliphatic substituents and enables good compatibility
of complex bioactive molecules. Furthermore, this is the first example
of photoinduced multicomponent reaction by employing bromodifluoroacetic
acid derivatives as a C1-synthon.
A novel and efficient three-component reaction with two C−N bonds and one C−F bond formation has been reported, which provides a straightforward route to a variety of fluorinated pyrimido[1,2-b]indazole derivatives. This transformation has the advantage of excellent functional group compatibility, including aliphatic and aromatic substituents enaminones. Moreover, metal and additives are not necessary for this reaction, which is of great significance for the synthesis and application of fluorinated heterocycles.
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