Medicine,
Journal Year:
2023,
Volume and Issue:
102(27), P. e34105 - e34105
Published: July 7, 2023
Background:
Recent
trials
have
highlighted
the
potential
of
oral
antiviral
VV116
in
treatment
patients
with
mild
COVID-19.
However,
no
comprehensive
studies
assessed
safety
and
efficacy
VV116.
Therefore,
we
conducted
a
systematic
review
to
assess
Methods:
A
search
was
on
PubMed,
Scopus,
Google
Scholar
websites,
cutoff
date
March
23,
identify
pertinent
studies.
Results:
The
results
from
3
included
indicated
that
serious
adverse
events
were
reported
experimental
groups,
which
exhibited
2.57-day
faster
time
viral
shedding
than
control
group
demonstrated
non-inferiority
nirmatrelvir-ritonavir
alleviating
major
symptoms.
Discussion:
Collectively,
available
suggest
reliable
profile
for
limited
number
insufficient
meta-analysis,
population
consisted
younger
individuals
moderate
symptoms,
not
encompassing
elderly
who
are
severely
affected
by
We
hope
more
will
be
future
ensure
has
clinical
setting,
especially
severe
or
critical
patients.
Angewandte Chemie International Edition,
Journal Year:
2024,
Volume and Issue:
63(27)
Published: March 21, 2024
The
importance
of
deuterium
labelling
in
a
variety
applications,
ranging
from
mechanistic
studies
to
drug-discovery,
has
spurred
immense
interest
the
development
new
methods
for
its
efficient
incorporation
organic,
and
especially
bioactive
molecules.
five-membered
heteroarenes
at
center
this
work
are
ubiquitous
motifs
molecules
these
compounds
therefore
highly
desirable.
However,
profound
differences
chemical
properties
encountered
between
different
hamper
single
set
broadly
applicable
reaction
conditions,
often
necessitating
separate
optimization
campaign
given
type
heteroarene.
In
study
we
describe
use
multi-substrate
screening
approach
identify
optimal
conditions
classes
minimal
number
reactions.
Using
approach,
four
sets
complementary
derived
our
dual
ligand-based
palladium
catalysts
nondirected
C(sp
Angewandte Chemie International Edition,
Journal Year:
2023,
Volume and Issue:
62(48)
Published: Sept. 20, 2023
Abstract
The
pharmacokinetics
of
pharmaceutical
drugs
can
be
improved
by
replacing
C−H
bonds
with
the
more
stable
C−D
at
α‐position
to
heteroatoms,
which
is
a
typical
metabolic
site
for
cytochrome
P450
enzymes.
However,
application
deuterated
synthons
limited.
Herein,
we
established
novel
concept
preparing
reagents
successful
synthesis
complex
drug
skeletons
deuterium
atoms
heteroatoms.
(
d
n
‐Alkyl)diphenylsulfonium
salts
prepared
from
corresponding
nondeuterated
forms
using
inexpensive
and
abundant
D
2
O
as
source
base,
were
used
electrophilic
alkylating
reagents.
Additionally,
these
sulfonium
efficiently
transformed
into
‐alkyl
halides
azide
coupling
amine
nucleophile.
Furthermore,
liver
microsomal
metabolism
studies
revealed
kinetic
isotope
effects
(KIE)
in
7‐(
‐ethoxy)flavone.
present
first
demonstration
KIE
‐ethoxy
group
will
contribute
discovery
research
based
on
chemistry.
Green Chemistry,
Journal Year:
2023,
Volume and Issue:
25(23), P. 9993 - 9997
Published: Jan. 1, 2023
An
efficient
electroselective
α-deuteration
of
amides
was
realized
via
H–D
exchange
under
mild
neutral
conditions.
Its
utility
has
been
well
exemplified
in
the
late-stage
modification
drug
molecules
and
transformation
to
β-bisdeuterated
amines.
Efficient
D
2
generation
is
crucial
for
synthesizing
deuterated
compounds.
Our
study
shows
that
forms
via
the
Grotthuss
mechanism
on
Pd/C,
where
O
and
H*
form
an
HD
O*
intermediate,
involving
proton–electron
transfer
from
H
to
metal
surface.
Organic Letters,
Journal Year:
2025,
Volume and Issue:
27(5), P. 1112 - 1117
Published: Jan. 23, 2025
The
Nozaki-Hiyama-Kishi
reaction
offers
effective
and
reliable
strategies
for
the
preparation
of
alcohols
via
carbon-carbon
bond
formation.
Typical
methods
usually
require
stoichiometric
amounts
chromium
salts,
co-transition
metals,
auxiliary
reagents,
which
limits
their
practical
application
in
industrial
chemistry.
To
mitigate
these
limitations,
substantial
efforts
have
been
made
to
develop
chromium-catalytic
approaches.
However,
an
excess
metal
reductants
or
expensive
photocatalysts
played
essential
roles
during
catalytic
cycles.
Here,
we
present
a
photoactive
electron
donor-acceptor
(EDA)
complex-induced
chromium-catalyzed
route,
accomplishing
alkyl
addition
aldehydes
without
requirement
photocatalysts.
Furthermore,
on
basis
pH-dependent
site-selective
hydrogen
isotope
exchange
thianthrenium
range
β-deuterated
secondary
could
be
prepared
with
high
efficiency
excellent
deuterium
incorporation.
Mechanistic
studies
revealed
that
photoinduced
intramolecular
single-electron
transfer
EDA
complex
happened
provide
radicals
are
captured
by
Cr(II)
species
facilitate
subsequent
Meanwhile,
excited
Hantzsch
ester
act
as
terminal
reductant
turnover
catalyst.
Nature Communications,
Journal Year:
2025,
Volume and Issue:
16(1)
Published: Feb. 3, 2025
Labelled
compounds
bearing
hydrogen
isotopes
are
keystones
in
diverse
areas
constituting
a
multi-billion
dollar
global
market
including
drugs,
diagnostics,
biology,
toxicology
and
smart
materials.
While
deuterium
exchange
(HDE)
methods
hold
promise
as
relevant
tools
for
the
late-stage
one-step
preparation
of
deuterium-labelled
compounds,
they
often
fall
short
achieving
sufficient
isotopic
purity
combined
either
with
site-selectivity
or
full
deuteration
process,
highlighting
need
further
development
optimisation.
This
report
pinpoints
an
approach
to
unlock
potential
HDE
using
concept
iterative
runs
continuous-flow
technology
(recirculation
process).
closed-loop
process
grants
access
now
deuterated
high
purities,
labelled
at
precise
site
perdeuterated
on
demand,
fast,
productive,
environmentally
friendly
way.
Hydrogen
but
process.
Here,
authors
technology.
