Metal‐Free Regioselective Direct C(4)−H Amination of Quinazoline with N‐fluorobenzenesulfonimide
ChemPlusChem,
Год журнала:
2024,
Номер
89(11)
Опубликована: Июль 18, 2024
Abstract
A
facile
C−H
amination
of
quinazoline
employing
N
‐fluorobenzenesulfonimide
(NFSI)
as
the
source
has
been
disclosed
in
absence
any
metal,
oxidant
or
additive.
The
methodology
shows
a
board
range
quinazolines
with
different
functional
groups
moderate
to
good
yields
up
87
%.
Furthermore,
gram‐scale
reaction,
desulfonylation
amine
and
synthesis
pharmaceutical
intermediate
were
also
investigated,
which
demonstrates
potential
applications
medicinal
chemistry.
plausible
mechanism
is
proposed
via
F
+
transfer
accompanied
by
removal
one
molecule
PhSO
2
F.
DFT
studies
experimental
work
suggest
that
more
favorable
than
free
radical
one.
Язык: Английский
A Portal to Highly Valuable Pyridonyl Vinyl Sulfonyl Fluorides and Aliphatic Sulfonyl Fluorides
Synthesis,
Год журнала:
2024,
Номер
unknown
Опубликована: Ноя. 18, 2024
Abstract
A
novel
and
efficient
method
for
selective
Michael
addition
of
2-pyridones
to
ethenesulfonyl
fluoride
(ESF)
1-bromoethene-1-sulfonyl
(BESF)
has
been
developed
constructing
a
class
pyridonyl
aliphatic
sulfonyl
fluorides
vinyl
in
good
excellent
yields.
This
practical
features
easy
operation,
wide
substrate
scope,
mild
reaction
conditions.
Язык: Английский
Cs2CO3‐Catalyzed Multi‐Component One‐Pot Stepwise Route for the Synthesis of Polysubstituted 2‐Pyridones
ChemistrySelect,
Год журнала:
2024,
Номер
9(45)
Опубликована: Ноя. 30, 2024
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.
Язык: Английский
Co(III) or Ru(II)-Catalyzed Selective C–H Alkynylation of 2-Pyridones and Their Derivatives with Bromoalkynes
The Journal of Organic Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Дек. 5, 2024
We
successfully
reported
selective
C–H
alkynylation
of
2-pyridones
with
bromoalkynes
under
the
catalysis
Co(III)
or
Ru(II).
The
reaction
used
easily
accessible
instead
high-valent
iodine
alkynes.
There
is
a
broad
substrate
scope
good
yields.
In
addition,
2-pyridone
can
be
as
weakly
directing
group
for
proximal
aryl
bond.
This
method
offers
an
efficient
approach
synthesizing
diverse
derivatives,
yielding
alkynylated
products
up
to
95%
yield
(>40
examples).
Язык: Английский