The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Dec. 26, 2024
In
this
work,
a
switchable
synthesis
of
β-ketosulfone
and
α-chloroketone
through
radical
difunctionalization
alkenes
is
reported.
The
transformation
works
well
under
iron
peroxo
species/photoredox
dual
catalysis
an
open-flask
atmosphere,
the
reaction
highlighted
with
good
yields
broad
scope.
Mechanism
studies
show
that
initiated
by
formal
[4
+
2]
cyclization
sulfonyl
in
regioselective
manner.
The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
89(5), P. 3509 - 3524
Published: Feb. 16, 2024
A
photocatalytic
annulation
cascade
of
unactivated
N-alkene-linked
indoles
with
Langlois'
reagent
by
a
radical
relay
is
developed
at
room
temperature
under
blue
LED
irradiation.
The
reaction
afforded
series
tri/difluoromethylated
pyrrolo[1,2-a]indoles
in
moderate
to
good
yields.
DFT
study
suggests
that
the
ascribed
rhodamine
6G-induced
cyclization
involving
vinyl
addition-radical
and
hydrogen-atom-abstraction
(HAA)
processes,
interestingly,
are
applied
as
fluorescent
dyes
into
fluorescence
spectrum
live-cell
imaging.
This
paper
represents
an
initial
example
on
cascades
HAA
process.
ACS Catalysis,
Journal Year:
2024,
Volume and Issue:
14(6), P. 4329 - 4339
Published: March 6, 2024
An
iron-catalyzed
lactonization
reaction
via
intramolecular
C(sp3)-H
functionalization
is
described.
The
process
employs
easily
accessible
hydroxamate
derivatives
from
which
the
noncommon
insertion
of
oxygen
occurred
through
a
1,5-hydrogen
atom
transfer.
A
mixture
water
and
hexafluoroisopropanol
as
solvent
appeared
to
be
key
parameter
this
transformation
reach
high
selectivity
efficiency.
Organic Letters,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 10, 2025
A
general
and
efficient
method
for
the
direct
alkynylation
oxidation
of
remote
C(sp3)-H
bonds
under
photoirradiation
is
described.
In
this
reaction,
Pd
catalyst
acts
as
both
a
photocatalyst
to
generate
nitrogen
radical
cross-coupling
with
terminal
alkyne.
Attractive
features
system
include
good
functional
group
tolerance,
scalability,
convenient
reagents,
an
operating
system.
The
utility
protocol
highlighted
by
its
application
derivatization
several
valuable
aza-heterocycles
such
caspase-3
inhibitor
azepinone
derivatives.
Chemical Communications,
Journal Year:
2023,
Volume and Issue:
59(89), P. 13309 - 13312
Published: Jan. 1, 2023
This
study
describes
an
iron-catalyzed
divergent
oxidation
of
styrene
into
β-hydroxylmethylketone
and
ketone
under
photo-irradiation.
divergence
is
ascribed
to
the
use
with
various
substituents.
More
importantly,
methanol
oxidized
formaldehyde
in
reaction
serves
as
a
C1
synthon.
Mechanism
investigations
show
that
initiated
by
oxidative
SET
transfer
cation
radical.
The
pathway
undergoes
HAT
β-hydride
elimination
well
concerted
cyclization.
Particularly,
several
drug-like
molecules,
such
melperone
analogue,
lenperone
haloperidol
are
synthesized.
In
addition,
this
method
also
applicable
synthesis
natural
product
(R)-atomoxetine.
bioRxiv (Cold Spring Harbor Laboratory),
Journal Year:
2024,
Volume and Issue:
unknown
Published: March 16, 2024
Abstract
Immunomodulatory
imide
drugs
(IMiDs)
including
thalidomide,
lenalidomide,
and
pomalidomide,
can
be
used
to
induce
degradation
of
a
protein
interest
that
is
fused
short
zinc
finger
(ZF)
degron
motif.
These
IMiDs,
however,
also
endogenous
neosubstrates,
IKZF1
IKZF3.
To
improve
selectivity,
we
took
bump-and-hole
approach
design
screen
bumped
IMiD
analogs
against
8380
ZF
mutants.
This
yielded
analog
induces
efficient
mutant
degron,
while
not
affecting
other
cellular
proteins,
In
proof-of-concept
studies,
this
system
was
applied
TRIM28,
disease-relevant
with
no
known
small
molecule
binders.
We
anticipate
will
make
valuable
addition
the
current
arsenal
systems
for
use
in
target
validation.
One-Sentence
Summary
Engineered
zinc-finger-based
degrons
enable
targeted
induced
by
selective
molecular
glues.
Synthesis,
Journal Year:
2023,
Volume and Issue:
56(03), P. 496 - 506
Published: Sept. 27, 2023
Abstract
A
photo-induced
intramolecular
electrophilic
aromatic
substitution
(SEAr)
of
N-acyloxyamides
using
FeCl3
in
1,4-dioxane
is
reported
for
the
synthesis
biologically
interesting
benzoxazin-3(4H)-ones.
It
believed
that
irradiation
with
a
blue
LED
facilitates
reaction,
serving
as
source
energy.
The
SEAr
reaction
pathway
ascribed
to
electronic
effects
present
aryl
ring
substrates.
also
applicable
useful
scaffolds
possessing
quinolin-2-one
core,
such
an
anticancer
reagent
and
analogues
brexipiprazole
cilostamide.
