The preparation of
phthalazinone derivatives is pivotal for their
utilization as pharmaceutical agents and other entities. Herein, we
report the phthalazinone-assisted carbon–nitrogen bond forming
reaction using dioxazolones as robust amidation sources under Rh(III)
catalysis. The broad functional group tolerance and complete site-selectivity
are observed. Notably, a series of transformations of synthesized
compounds into biologically relevant N-heterocycles
demonstrates the applicability of the developed methodology.
Ruthenium(II)-catalyzed C(sp 2 )−H functionalization of N-aryl phthalazinones with a range of aldehydes and activated ketone is described. Initial formation of hydroxyalkylated phthalazinones and subsequent Mitsunobu cyclization provided facile access to biologically relevant indazolophthalazinones. The utility of this method is highlighted by synthetic transformations into a series of potentially bioactive scaffolds.
The ruthenium(II)-catalyzed cross-coupling reaction between 2-aryl quinazolinones and activated aldehydes is described. The method enables the site‐selective hydroxyalkylation under redox-neutral conditions. Moreover, this protocol provides a facile access to various...
The
facile synthesis of hydroxymethylated indole derivatives is
crucial for their further development as pharmaceutical compounds
and other synthetic purposes. Herein, we describe the ruthenium(II)-catalyzed
hydroxymethylation of indolines and other N-heterocycles using paraformaldehyde
as an abundant C1 feedstock. A wide substrate scope range and high
levels of site selectivity as well as functional group tolerance were
observed.
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