Catalysts,
Journal Year:
2022,
Volume and Issue:
12(5), P. 510 - 510
Published: May 2, 2022
C−H
methylation
of
sp2
and
sp3
carbon
centers
is
significant
in
many
biological
processes.
Methylated
drug
candidates
show
unique
properties
due
to
the
change
solubility,
conformation
metabolic
activities.
Several
photo-catalyzed,
electrochemical,
mechanochemical
metal-free
techniques
that
are
widely
utilized
strategies
medicinal
chemistry
for
arenes
heteroarenes
have
been
covered
this
review.
Chemistry - A European Journal,
Journal Year:
2023,
Volume and Issue:
29(72)
Published: Oct. 6, 2023
Direct
C-H
methylation
is
a
highly
valuable
approach
for
introducing
methyl
groups
into
organic
molecules,
particularly
in
pharmaceutical
chemistry.
Among
the
various
methodologies
available,
photo-induced
stands
out
as
an
exceptional
choice
due
to
its
mild
reaction
conditions,
energy
efficiency,
and
compatibility
with
functional
groups.
This
article
offers
comprehensive
review
of
photochemical
strategies
employed
direct
selective
C(sp3
)-H,
C(sp2
C(sp)-H
bonds
molecules.
The
discussed
encompass
transition-metal-based
photocatalysis,
organophotocatalysis,
well
other
metal-free
approaches,
including
electron
donor-acceptor
(EDA)-enabled
transformations.
Importantly,
wide
range
easily
accessible
agents
such
tert-butyl
peroxide,
methanol,
DMSO,
ether,
TsOMe,
N-(acetoxy)phthalimide,
acetic
acid,
halides,
even
methane
can
serve
effective
methylating
reagents
modifying
diverse
targets.
These
advancements
are
anticipated
drive
further
progress
fields
synthesis,
development,
opening
up
exciting
avenues
creating
novel
molecules
discovering
new
drug
compounds.
The Journal of Organic Chemistry,
Journal Year:
2021,
Volume and Issue:
86(7), P. 4932 - 4943
Published: March 17, 2021
A
convenient
preparation
method
of
N-acylbenzoxazines
has
been
developed,
in
which
phenols
react
with
nitriles
and
dimethyl
sulfoxide
(DMSO)
the
presence
a
catalytic
amount
(COCl)2
CH3CN
or
chloroform
to
afford
corresponding
moderate-to-good
yields.
DMSO
acts
as
source
HCHO,
is
generated
situ
from
decomposition
methoxydimethylsulfonium
salt.
regeneration
cycle
salt
proposed,
initiated
by
(COCl)2.
Angewandte Chemie International Edition,
Journal Year:
2024,
Volume and Issue:
63(51)
Published: Sept. 5, 2024
Benzo[1,3,2]dithiazole-1,1,3-trioxides
are
bench-stable
and
easy-to-use
reagents.
In
photoredox
catalysis,
they
generate
methyl
perdeuteromethyl
radicals
which
can
add
to
a
variety
of
radical
acceptors,
including
olefins,
acrylamides,
quinoxalinones,
isocyanides,
enol
silanes,
N-Ts
acrylamide.
As
byproduct,
salt
is
formed
be
regenerated
the
original
methylating
agent.
Flow
chemistry
provides
an
option
for
reaction
scale-up
further
underscoring
synthetic
usefulness
these
methylation
Mechanistic
investigations
suggest
single-electron
transfer
(SET)
pathway
induced
by
catalysis.
The Journal of Organic Chemistry,
Journal Year:
2019,
Volume and Issue:
85(2), P. 508 - 514
Published: Nov. 29, 2019
Using
a
hydrogen-transfer-mediated
activation
mode,
we
report
new
catalytic
system
for
the
transfer
hydrogenation
of
naphthols.
In
presence
Pd/C
catalyst
and
base,
various
naphthols
reacted
with
indolines
to
afford
N-aryl-substituted
heterocyclic
compounds.
Indolines
were
found
act
as
novel
hydrogen
donors
under
palladium
catalysis.
This
method
features
good
functional
tolerance,
operational
simplicity,
readily
available
catalyst.
Catalysts,
Journal Year:
2022,
Volume and Issue:
12(5), P. 510 - 510
Published: May 2, 2022
C−H
methylation
of
sp2
and
sp3
carbon
centers
is
significant
in
many
biological
processes.
Methylated
drug
candidates
show
unique
properties
due
to
the
change
solubility,
conformation
metabolic
activities.
Several
photo-catalyzed,
electrochemical,
mechanochemical
metal-free
techniques
that
are
widely
utilized
strategies
medicinal
chemistry
for
arenes
heteroarenes
have
been
covered
this
review.