Abstract
We
report
a
catalyst-free
intermolecular
hydride-transfer
reaction
to
synthesize
N-benzylindolines
under
microwave
heating
in
the
absence
of
solvent.
The
reactions
are
performed
by
taking
indoline
(two
equivalents)
with
aryl
aldehydes,
which
give
good
yields
products.
Tetrahydroisoquinoline
can
also
be
used
place
excellent
expected
A
mechanism
has
been
proposed.
antioxidant
properties
all
were
tested
and
compared
that
ascorbic
acid,
showing
some
them
powerful
antioxidants.
RSC Advances,
Год журнала:
2024,
Номер
14(8), С. 5547 - 5565
Опубликована: Янв. 1, 2024
Spiro
heterocycle
frameworks
are
a
class
of
organic
compounds
that
possesses
unique
structural
features
making
them
highly
sought-after
targets
in
drug
discovery
due
to
their
diverse
biological
and
pharmacological
activities.
Scientific Reports,
Год журнала:
2024,
Номер
14(1)
Опубликована: Янв. 4, 2024
Abstract
Hybrid
molecules
maintain
their
stronghold
in
the
drug
market,
with
over
60%
of
candidates
pharmaceutical
industries.
The
substantial
expenses
for
developing
and
producing
biologically
privileged
drugs
are
expected
to
create
opportunities
hybrid
molecule-based
drugs.
Therefore,
we
have
developed
a
simple
efficient
copper-catalyzed
approach
synthesizing
wide
range
triazole-linked
glycohybrids
derived
from
pyrazolo[1,5-
]pyrimidines.
Employing
microwave-assisted
approach,
concise
route
using
various
7-
O
-propargylated
]pyrimidines
1-azidoglycosides.
This
strategy
afforded
series
twenty-seven
up
98%
yield
diverse
stereochemistry.
All
were
achieved
within
remarkably
shortened
time
frame.
Our
investigation
extends
evaluating
anticancer
potential
these
synthesized
]
pyrimidine-based
glycohybrids.
In-vitro
assays
against
MCF-7,
MDA-MB231,
MDA-MB453
cell
lines
reveal
intriguing
findings.
(
2R,3S,4S,5R,6R
)-2-(acetoxymethyl)-6-(4-(((5-(4-chlorophenyl)pyrazolo[1,5-
]pyrimidin-7-yl)oxy)methyl)-1
H
-1,2,3-triazol-1-yl)tetrahydro-2
-pyran-3,4,5-triyl
triacetate
emerges
as
standout
better
activity
MDA-MB231
cells
(IC
50
=
29.1
µM),
while
2R,3R,4S,5R,6R
demonstrates
best
inhibitory
effects
MCF-7
15.3
µM)
all
compounds.
These
results
align
our
docking
analysis
structure–activity
relationship
(SAR)
investigations,
further
validating
in-vitro
outcomes.
work
not
only
underscores
synthetic
utility
devised
protocol
but
also
highlights
promising
therapeutic
exploration.
Abstract
This
study
presents
a
microwave‐assisted,
metal‐free
approach
for
the
fast
and
selective
synthesis
of
pyridine‐functionalized
N
‐heterocyclic
ligand
precursors.
Efficient
synthetic
methods
are
important
in
development
cost‐effective
transition
metal
complexes
commonly
used
as
catalysts
various
applications.
Traditional
forming
C–N
C–C
bonds
require
long
reaction
times
harsh
conditions,
whereas
microwave
heating
accelerates
by
significantly
reducing
time
temperature,
under
metal‐
additive‐free
conditions.
has
enabled
mono‐
di‐substituted
pyridine‐based
synthons
starting
from
2,6‐dibromopyridine
well
2,6‐dichloropyridine.
The
also
applies
to
other
substrates,
delivering
high‐purity
ligands
5–15
min.
Notably,
this
method
provides
an
alternative
cross‐coupling
reactions,
eliminating
requirement
copper
catalysts,
more
sustainable
efficient
conventional
strategies.
prepared
using
microwave‐assisted
reported
here
have
been
utilized
prepare
some
common
preparation
organometallic
complexes.
