Synlett,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Nov. 22, 2024
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,
Journal Year:
2024,
Volume and Issue:
14(8), P. 5547 - 5565
Published: Jan. 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,
Journal Year:
2024,
Volume and Issue:
14(1)
Published: Jan. 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.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(24), P. 8152 - 8152
Published: Dec. 18, 2023
The
molecular
mechanism
of
the
[3+2]
cycloaddition
reactions
between
aryl
azides
and
ethyl
propiolate
was
evaluated
in
framework
Molecular
Electron
Density
Theory.
It
found
that
independently
nature
substituent
within
azide
molecule,
process
is
realized
via
a
polar
but
single-step
mechanism.
All
attempts
localization
as
postulated
earlier
by
Abu-Orabi
coworkers'
zwitterionic
intermediates
were
not
successful.
At
same
time,
formation
zwitterions
with
an
"extended"
conformation
possible
on
parallel
reaction
paths.
ELF
analysis
shows
studied
leading
to
1,4-triazole
proceeds
two-stage
one-step
also
revealed
both
are
created
donation
nitrogen
atom's
nonbonding
electron
densities
carbon
atoms
propiolate.
Chemistry - A European Journal,
Journal Year:
2024,
Volume and Issue:
30(47)
Published: Aug. 2, 2024
Abstract
The
Kröhnke
Pyridine
Synthesis
has
been
discovered
about
six
decades
ago
(1961),
by
Fritz
and
Wilfried
Zecher
at
the
University
of
Giessen.
original
method
involved
reaction
α‐pyridinium
methyl
ketone
salts
with
α,β‐unsaturated
carbonyl
compounds
in
presence
a
nitrogen
source,
frequently
ammonium
acetate.
Since
its
discovery,
methodology
demonstrated
to
be
suitable
for
preparation
mono‐,
di‐,
tri‐
tetra‐pyridines,
important
applications
several
research
fields.
Over
years,
number
modifications
approach
have
developed
reported,
enabling
broad
applicability
these
methods
even
modern
days,
also
synthesis
non‐pyridine
compounds.
In
this
critical
tutorial
review,
we
will
thoroughly
explore
discuss
potential
method,
refinements
that
made
over
as
well
some
arising
from
each
type
pyridine
and/or
produced
Kröhnke's
approach.
