Abstract
A
concise
and
practicable
route
to
the
synthesis
of
multisubstituted
2‐pyridones
via
a
four‐component
one‐pot
stepwise
cyclization
catalyzed
by
Cs
2
CO
3
has
been
developed.
During
this
transformation,
two
new
C‐C
bonds
C‐N
were
generated
through
an
intermolecular
condensation/aza‐Michael
reaction/intermolecular
Michael
addition/intramolecular
sequence.
The
alternative
protocol
offers
complementary
provide
series
structurally
diverse
polysubstituted
(21
examples)
in
good
excellent
yields
(52–81%)
from
easily
available
raw
materials
arylamines,
dialkyl
acetylenedicarboxylate,
1,3‐dicarbonyl
compounds,
trialkyl
orthoformate
under
mild
conditions.
It
might
opportunities
for
discovery
2‐pyridones‐containing
drugs.
Organic Chemistry Frontiers,
Год журнала:
2024,
Номер
unknown
Опубликована: Янв. 1, 2024
This
method
provides
an
effective
means
for
the
1,2-selective
arylamination
of
1,3-dienes,
demonstrating
a
wide
substrate
scope
and
excellent
functional
group
tolerance
solving
problem
poor
selectivity
in
dienes.
Abstract
A
concise
and
practicable
route
to
the
synthesis
of
multisubstituted
2‐pyridones
via
a
four‐component
one‐pot
stepwise
cyclization
catalyzed
by
Cs
2
CO
3
has
been
developed.
During
this
transformation,
two
new
C‐C
bonds
C‐N
were
generated
through
an
intermolecular
condensation/aza‐Michael
reaction/intermolecular
Michael
addition/intramolecular
sequence.
The
alternative
protocol
offers
complementary
provide
series
structurally
diverse
polysubstituted
(21
examples)
in
good
excellent
yields
(52–81%)
from
easily
available
raw
materials
arylamines,
dialkyl
acetylenedicarboxylate,
1,3‐dicarbonyl
compounds,
trialkyl
orthoformate
under
mild
conditions.
It
might
opportunities
for
discovery
2‐pyridones‐containing
drugs.
