Research Square (Research Square),
Год журнала:
2023,
Номер
unknown
Опубликована: Июнь 13, 2023
Abstract
Metallaphotocatalysis
has
been
recognized
as
a
pivotal
catalysis
for
enabling
new
reactivities
and
expanding
chemical
space.
Traditional
metallaphotocatalysis
often
requires
two
or
more
separate
catalysts
exhibits
flaw
in
cost
substrate-tolerance,
thus
representing
an
await-to-solve
issue
catalysis.
We
herein
realize
with
bifunctional
dirhodium
tetracarboxylate
([Rh2])
alone.The
[Rh2]
shows
unprecedente
photocatalytic
activity
via
rarely
used
metal-to-metal
transition
photocatalysis.
Based
on
the
activity,
connects
carbene
chemistry
siglet
oxygen
to
enable
novel
photochemical
cascde
reaction
(PCR).
The
PCR
is
characterized
by
high
atom-efficiency,
excellent
stereoselectivities,
mild
conditions,
scalable
synthesis,
valuable
products.
DFT
calculations-aided
mechanistic
study
rationalizes
pathway
interprets
stereoselectivities
of
PCR.
products
showed
inhibitory
against
PTP1B,
being
promising
treatment
type
II
diabetes
cancers.
believe
this
work
will
shed
light
discovering
developing
PCRs
exploring
Communications Chemistry,
Год журнала:
2024,
Номер
7(1)
Опубликована: Июнь 12, 2024
The
discovery
of
selective
Nav1.7
inhibitors
is
a
promising
approach
for
developing
anti-nociceptive
drugs.
In
this
study,
we
present
novel
oxindole-based
readily
accessible
library
(OREAL),
which
characterized
by
accessibility,
unique
chemical
space,
ideal
drug-like
properties,
and
structural
diversity.
We
used
scaffold-based
to
screen
the
OREAL
discovered
compound
C4
as
potent
inhibitor.
bioactivity
characterization
reveals
that
it
inhibitor
effectively
reverses
Paclitaxel-induced
neuropathic
pain
(PINP)
in
rodent
models.
Preliminary
toxicology
study
shows
negative
hERG.
consistent
results
molecular
docking
simulations
further
support
reasonability
in-silico
screening
show
insight
binding
mode
C4.
Our
paves
way
pushing
Nav1.7-based
drugs
forward
clinic.
Advanced Synthesis & Catalysis,
Год журнала:
2024,
Номер
366(17), С. 3616 - 3623
Опубликована: Июнь 20, 2024
Abstract
A
three‐component
allylic
alkylation
reaction
of
α‐diazo
ketones,
water
and
allyl
carbonate
under
the
cooperative
catalysis
Rh
2
(OAc)
4
,
Pd
(dba)
3
Brønsted
acid
was
disclosed.
This
method
provides
an
expeditious
access
to
α‐keto
homoallylic
alcohols
in
good
high
yields.
Controlled
experiments
support
that
transformations
proceed
through
cross‐interception
two
active
intermediates
Pd‐allyl
species
enol
derived
from
oxonium
ylides.
Moreover,
synthetic
generated
products
enable
creation
motifs
enriched
with
dense
functional
groups,
underscoring
their
potential
as
valuable
building
blocks.
Research Square (Research Square),
Год журнала:
2024,
Номер
unknown
Опубликована: Сен. 16, 2024
Abstract
Multi-component
multi-functionalization
reactions
involving
active
intermediates
are
powerful
tools
for
rapidly
generating
a
wide
array
of
compounds.
Metal
carbynoids,
with
their
distinct
reactivity,
hold
great
promise
developing
new
synthetic
methodologies.
However,
application
in
catalytic
transfer
has
been
hindered
by
the
limited
availability
suitable
precursors.
In
this
study,
we
investigate
potential
α-halo
Rh-carbenes,
leveraging
concept
metal
carbynoids
reactions.
Through
chiral
phosphoric
acid-catalyzed
asymmetric
trifunctionalization,
have
developed
an
innovative
method
synthesizing
variety
α-cyclic
ketal
β-amino
esters
high
yields
and
excellent
enantioselectivity.
Our
extensive
experimental
computational
studies
reveal
that
Rh-carbenes
exhibit
carbynoid
properties,
which
facilitate
transformation
into
functionalized
Fischer-type
through
decomposition
C-halo
bond.
Research Square (Research Square),
Год журнала:
2023,
Номер
unknown
Опубликована: Июнь 13, 2023
Abstract
Metallaphotocatalysis
has
been
recognized
as
a
pivotal
catalysis
for
enabling
new
reactivities
and
expanding
chemical
space.
Traditional
metallaphotocatalysis
often
requires
two
or
more
separate
catalysts
exhibits
flaw
in
cost
substrate-tolerance,
thus
representing
an
await-to-solve
issue
catalysis.
We
herein
realize
with
bifunctional
dirhodium
tetracarboxylate
([Rh2])
alone.The
[Rh2]
shows
unprecedente
photocatalytic
activity
via
rarely
used
metal-to-metal
transition
photocatalysis.
Based
on
the
activity,
connects
carbene
chemistry
siglet
oxygen
to
enable
novel
photochemical
cascde
reaction
(PCR).
The
PCR
is
characterized
by
high
atom-efficiency,
excellent
stereoselectivities,
mild
conditions,
scalable
synthesis,
valuable
products.
DFT
calculations-aided
mechanistic
study
rationalizes
pathway
interprets
stereoselectivities
of
PCR.
products
showed
inhibitory
against
PTP1B,
being
promising
treatment
type
II
diabetes
cancers.
believe
this
work
will
shed
light
discovering
developing
PCRs
exploring