Journal of Fluorine Chemistry,
Год журнала:
2023,
Номер
273, С. 110239 - 110239
Опубликована: Дек. 30, 2023
Fluorinated
molecules
often
show
superior
bioactivity
or
ADME
(absorption,
distribution,
metabolism,
and
excretion)
properties
compared
to
their
non-fluorinated
analogues.
In
fact,
20–30
%
of
newly
approved
drugs
the
majority
recently
agrochemicals
are
organofluorine
compounds.
Unsurprisingly,
there
is
great
interest
in
development
new
and/or
improved
processes
for
fluorine
incorporation.
Pd-catalyzed
arylfluorination
alkenes
a
novel,
emerging
fluorination
method,
which
simultaneously
introduces
atom
an
aryl
group
into
alkene
framework.
The
aim
current
work
was
studying,
improving,
extending
literature
protocol,
originally
utilized
N-allylated
sulfonamide
substrates.
Scientific Reports,
Год журнала:
2025,
Номер
15(1)
Опубликована: Фев. 28, 2025
The
DfrA1
protein
provides
trimethoprim
resistance
in
bacteria,
especially
Klebsiella
pneumoniae
and
Escherichia
coli,
by
modifying
dihydrofolate
reductase,
which
reduces
the
binding
efficacy
of
antibiotic.
This
study
identified
inhibitors
trimethoprim-resistant
through
high-throughput
computational
screening
optimization
3,601
newly
synthesized
chemical
compounds
from
ChemDiv
database,
aiming
to
discover
potential
drug
candidates
targeting
K.
E.
coli.
Through
this
approach,
we
six
promising
DCs,
labeled
DC1
DC6,
as
DfrA1.
Each
DC
showed
a
strong
ability
bind
effectively
formed
favorable
interactions
at
sites.
These
were
comparable
those
Iclaprim,
well-known
antibiotic
effective
against
To
confirm
our
findings,
explored
how
DCs
work
molecular
level,
focusing
on
their
thermodynamic
properties.
Additionally,
dynamics
simulations
confirmed
these
inhibit
protein.
Our
results
that
DC4
(an
organofluorinated
compound)
DC6
(a
benzimidazole
exhibited
than
control
drug,
particularly
regarding
stability,
solvent-accessible
surface
area,
solvent
exposure,
polarity,
site
interactions,
influence
residence
time
efficacy.
Overall,
findings
suggest
have
act
DfrA1,
offering
prospects
for
treatment
management
infections
caused
coli
both
humans
animals.
However,
further
vitro
validations
are
necessary.
The Chemical Record,
Год журнала:
2023,
Номер
23(9)
Опубликована: Май 23, 2023
Over
the
last
years,
methods
devoted
to
synthesis
of
asymmetric
molecules
bearing
a
perfluoroalkylated
chain
have
been
limited
in
number.
Among
them,
only
few
can
be
used
on
large
variety
scaffolds.
This
microreview
aims
at
summarizing
these
recent
advances
enantioselective
perfluoroalkylation
(-CF3
,
-CF2
H,
-Cn
F2n+1
)
and
highlights
need
for
new
easily
synthesize
chiral
fluorinated
which
would
useful
pharmaceutical
agrochemical
industries.
Some
perspectives
are
also
mentioned.
The Journal of Organic Chemistry,
Год журнала:
2021,
Номер
87(1), С. 670 - 682
Опубликована: Дек. 10, 2021
Enantiopure
fluorine
containing
β-amino
acids
are
of
large
biological
and
pharmaceutical
interest.
Strategies
to
prepare
acid
derivatives
possessing
a
F-containing
tetrasubstituted
stereocenter
at
the
α-C
atom
in
catalytic
asymmetric
sense
rare,
particular
using
an
enantioselective
electrophilic
C-F
bond
formation.
In
present
study,
highly
palladacycle-catalyzed
fluorination
isoxazolinones
was
developed.
It
is
demonstrated
that
useful
precursors
toward
enantiopure
by
diastereo-
chemoselective
reduction.
The
formed
γ-aminoalcohols
served
as
valuable
acids,
esters,
β-lactams,
all
featuring
fluorinated
stereocenters.
addition,
this
work,
enantioenriched
azetidines
were
accessible
for
first
time.
Chemistry - An Asian Journal,
Год журнала:
2022,
Номер
17(15)
Опубликована: Май 18, 2022
Due
to
the
increasing
relevance
of
fluorine-containing
organic
molecules
in
drug
design,
synthesis
organofluorine
compounds
has
gained
high
significance
synthetic
chemistry.
Trifluoromethylative
difunctionalizations
carbon-carbon
multiple
bonds,
with
simultaneous
incorporation
a
CF3
group
and
another
functional
element,
have
considerable
potential.
Because
importance
bond-forming
reactions
synthesis,
carbotrifluoromethylations
and,
particular,
aryltrifluoromethylations
or
heteroaryltrifluoromethylations
are
considered
be
fields
The
aim
current
review
is
summarize
recent
developments
aryltrifluoromethylation
heteroaryltrifluoromethylation
reactions.
Chemistry - A European Journal,
Год журнала:
2022,
Номер
28(63)
Опубликована: Авг. 9, 2022
Fluorine
incorporation
into
organic
molecules
is
often
beneficial
to
their
absorption,
distribution,
metabolism,
and
excretion
(ADME)
properties
or
bioactivity.
As
a
consequence,
organofluorine
compounds
have
become
quite
common
amongst
drugs
agrochemicals,
preparation
highly
important
topic
in
both
synthetic
chemistry
pharmaceutical
chemistry.
One
of
the
newly
developed
methods
for
accessing
Pd-catalyzed
arylfluorination
alkenes.
It
an
olefin
difunctionalization
process
that
simultaneously
introduces
aryl
group
fluorine
atom
alkene
framework.
This
review
provides
concise
overview
this
powerful
versatile
method.
Advanced Synthesis & Catalysis,
Год журнала:
2024,
Номер
366(6), С. 1412 - 1421
Опубликована: Янв. 23, 2024
Abstract
We
demonstrate
the
application
of
chiral
magnesium
complexes
in
an
asymmetric
carbon‐sulfur
bond‐forming
reaction.
Enantioselective
and
cost‐effective
methodology
under
mild
condition
for
thia‐Michael
addition,
utilizing
situ
generated
dinuclear
magnesium‐ProPhenol
complex,
has
been
developed.
The
versatility
this
protocol
is
demonstrated
with
a
broad
range
thiol
nucleophiles
wide
selection
enones.
Enantioenriched
β‐ketosulfides
are
obtained
good
to
excellent
yields
moderate
enantioselectivity.
presented
catalytic
system
exhibits
tolerance
structurally
different
substrates
while
maintaining
high
This
observation
aligns
proposed
mechanism,
wherein
sulfur
atom
coordinates
catalyst
close
proximity
reaction
center.
The Chemical Record,
Год журнала:
2023,
Номер
23(9)
Опубликована: Янв. 12, 2023
Abstract
The
chemistry
of
fluorinated
compounds
has
experienced
extraordinary
growth
in
recent
decades
due
to
the
many
and
varied
properties
which
that
contain
groups
possess.
Among
all
them,
chiral
imines,
particular
Ellman's
are
great
importance
since
they
some
most
interesting
building
blocks
for
synthesis
a
large
number
enantioenriched
carbocycles
heterocycles
with
biological
synthetic
properties.
This
personal
account
covers
significant
results
obtained
our
research
group
last
two
concerning
asymmetric
tandem
reactions,
paying
special
attention
intramolecular
aza‐Michael
reaction
(IMAMR),
diversity
oriented
(DOS),
reactions
involving
p‐tolylsulfinyl
as
inducer
cycloaddition
processes,
particular,
Pauson‐Khand
reaction,
[2+2+2]‐cycloadditions
metathesis
starting
mainly
from
enyne
through
use
N‐sulfinyl
imines
their
derivatives
materials.
The Journal of Organic Chemistry,
Год журнала:
2022,
Номер
87(11), С. 7291 - 7307
Опубликована: Май 18, 2022
C-7-fluorinated
derivatives
of
two
important
polyhydroxylated
pyrrolizidines,
casuarine
and
australine,
were
synthesized
with
organocatalytic
stereoselective
α-fluorination
aldehydes
as
the
key
step.
The
strategy
is
extensively
applicable
to
some
synthetically
challenging
fluorinated
iminosugars
carbohydrates.
docking
studies
indicated
that
potent
inhibitions
trehalase
amyloglucosidase
by
pyrrolizidines
are
due
interaction
modes
dominated
fluorine
atoms
in
these
amino
acids'
residues
corresponding
enzymes.
Steady
interactions
established
between
C-7
fluoride
a
hydrophobic
pocket
untypical
anion-π
interactions.
These
unexpected
related
structure-activity
relationship
emphasize
value
fluorination
design
pyrrolizidine
glycosidase
inhibitors.
