Organic Letters,
Год журнала:
2024,
Номер
26(3), С. 751 - 756
Опубликована: Янв. 12, 2024
A
highly
diastereoselective
[3
+
2]
cycloaddition
of
aziridines
with
difluorinated
silyl
enol
ethers
has
been
developed.
This
approach
provides
a
facile
methodology
for
functionalized
gem-difluorinated
pyrrolidines
in
good
to
excellent
yields
functional
group
tolerance.
one-pot,
two-step
synthesis
structurally
interesting
fluorinated
pyrroles
also
developed
through
cycloaddition/aromatization/desulfonation
sequence.
Moreover,
readily
available
substrates,
mild
reaction
conditions,
and
easy
scale-up
show
practical
advantages.
Arabian Journal of Chemistry,
Год журнала:
2022,
Номер
15(11), С. 104242 - 104242
Опубликована: Сен. 13, 2022
Human
immunodeficiency
virus
(HIV)
especially
HIV-1
infection
and
its
progression
to
acquired
immune
deficiency
syndrome
(AIDS)
remains
a
significant
global
health
challenge.
The
advent
of
the
highly
active
antiretroviral
therapy
(HAART)
has
greatly
extended
life
expectancy
patients
living
with
HIV,
but
it
become
evident
that
long-term
HAART
will
not
eliminate
HIV
reservoir
cure
infection.
Moreover,
drug
resistance
undesirable
side
effects
hamper
efficacious
therapy,
creating
an
urgent
need
develop
novel,
more
effective
less
toxic
anti-HIV
therapeutics.
Imidazole,
oxazole
thiazole
two
heteroatoms
at
meta-position
five-membered
rings
are
fascinating
structures
constitute
important
class
heterocycles
in
discovery.
Their
derivatives
could
exert
activity
through
diverse
mechanisms
possess
promising
antiviral
against
both
drug-sensitive
drug-resistant
strains.
This
review
summarizes
research
progress
made
regarding
potential
imidazole,
hybrids,
structure–activity
relationships
(SARs)
also
discussed
facilitate
further
rational
design
candidates,
covering
articles
published
from
2012
2022.
Chemical Biology & Drug Design,
Год журнала:
2022,
Номер
100(5), С. 682 - 698
Опубликована: Сен. 5, 2022
Histone-modifying
enzymes
are
the
key
regulators
involved
in
post-translational
modification
of
histone
and
non-histone.
These
responsible
for
epigenetic
control
cellular
functions.
However,
deregulation
activity
these
results
uncontrolled
disorders
such
as
cancer
inflammatory
neurological
diseases.
The
study
includes
acetyltransferases,
deacetylases,
methyl
transferases,
demethylases,
DNA
their
potent
inhibitors
which
a
clinical
trial
used
medicinal
drugs.
present
review
covers
heterocycles
target-specific
histone-modifying
enzyme,
more
specifically
acetyltransferases.
This
also
confers
recent
reports
on
potential
HAT
covered
from
2016
to
2022
future
perspectives
therapy.
Angewandte Chemie International Edition,
Год журнала:
2023,
Номер
62(25)
Опубликована: Апрель 7, 2023
A
concise
asymmetric
total
synthesis
of
(-)-quinocarcin
has
been
accomplished
with
high
step
economy
from
commercially
available
starting
materials.
catalytic
enantioselective
reductive
1,3-dipolar
cycloaddition
reaction
N-heteroaryl
secondary
amides
reactive
dipolarophiles
using
iridium/copper
relay
catalysis
was
developed
to
prepare
the
key
chiral
pyrrolidine
intermediate
three
stereocenters.
This
protocol
features
excellent
regio-,
exo-
and
enantioselectivities,
broad
substrate
scope,
good
functional
group
tolerance.
The
efficiency
also
ensured
by
a
RhIII
-catalyzed
C-H
activation/cyclization
tandem
diastereoselective
hydrogenation/cyclization
construct
tetrahydroisoquinoline-pyrrolidine
tetracyclic
core
unit
quinocarcin.
Organic Letters,
Год журнала:
2024,
Номер
26(3), С. 751 - 756
Опубликована: Янв. 12, 2024
A
highly
diastereoselective
[3
+
2]
cycloaddition
of
aziridines
with
difluorinated
silyl
enol
ethers
has
been
developed.
This
approach
provides
a
facile
methodology
for
functionalized
gem-difluorinated
pyrrolidines
in
good
to
excellent
yields
functional
group
tolerance.
one-pot,
two-step
synthesis
structurally
interesting
fluorinated
pyrroles
also
developed
through
cycloaddition/aromatization/desulfonation
sequence.
Moreover,
readily
available
substrates,
mild
reaction
conditions,
and
easy
scale-up
show
practical
advantages.
