Organic Process Research & Development,
Journal Year:
2023,
Volume and Issue:
28(5), P. 1567 - 1575
Published: Sept. 11, 2023
A
new
and
highly
efficient
continuous
flow
process
is
presented
for
the
synthesis
of
aziridines
via
thermal
Baldwin
rearrangement.
The
was
initially
explored
using
traditional
batch
techniques
but
suffered
from
moderate
yields,
long
reaction
times,
diastereoselectivities.
Here
we
demonstrate
that
can
be
greatly
improved
upon
its
transfer
to
flow,
which
afforded
aziridine
targets
in
high
short
consistently
diastereoselectivities,
with
high-throughput
rendering
multigram
quantities
product
periods
time.
In
addition,
processing
extended
substrate
scope
including
several
examples
had
failed
mode,
thus
demonstrating
value
this
overlooked
entry
into
valuable
species.
Frontiers in Chemistry,
Journal Year:
2024,
Volume and Issue:
12
Published: Feb. 19, 2024
This
comprehensive
review,
covering
2021-2023,
explores
the
multifaceted
chemical
and
pharmacological
potential
of
coumarins,
emphasizing
their
significance
as
versatile
natural
derivatives
in
medicinal
chemistry.
The
synthesis
functionalization
coumarins
have
advanced
with
innovative
strategies.
enabled
incorporation
diverse
functional
fragments
or
construction
supplementary
cyclic
architectures,
thereby
biological
physico-chemical
properties
compounds
obtained
were
enhanced.
unique
structure
coumarine
facilitates
binding
to
various
targets
through
hydrophobic
interactions
pi-stacking,
hydrogen
bonding,
dipole-dipole
interactions.
Therefore,
this
important
scaffold
exhibits
promising
applications
uncountable
fields
chemistry
(e.g.,
neurodegenerative
diseases,
cancer,
inflammation).
The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
89(5), P. 3251 - 3258
Published: Feb. 15, 2024
Aziridines
are
important
structural
motifs
and
intermediates,
several
synthetic
strategies
for
the
direct
aziridination
of
alkenes
have
been
introduced.
However,
many
these
require
an
excess
activated
alkene,
suffer
from
competing
side-reactions,
limited
functional
group
tolerance,
or
involve
precious
transition
metal-based
catalysts.
Herein,
we
demonstrate
by
combining
sulfonyl
azides
as
a
triplet
nitrene
source
with
catalytic
amount
organic
dye
functioning
photosensitizer.
We
show
how
nature
azide,
in
combination
triplet-excited
state
energy
photosensitizer,
affects
yield
provide
mechanistic
rationale
to
account
observed
dependence
reaction
on
azide
reagents.
The
optimized
conditions
enable
structurally
diverse
complex
alkenes,
carrying
various
groups,
alkene
limiting
reagent.
Catalysis Science & Technology,
Journal Year:
2024,
Volume and Issue:
14(18), P. 5143 - 5160
Published: Jan. 1, 2024
This
review
article
summarizes
the
visible
light
mediated
synthesis
of
allenes
from
substrates
like
1,3-enynes,
propargylic
carbonates,
homopropargylic
alcohols,
oxalates,
alkynyl
diazo
compounds,
and
terminal
aziridines.
ACS Catalysis,
Journal Year:
2024,
Volume and Issue:
14(16), P. 12310 - 12317
Published: Aug. 2, 2024
Aziridines
are
important
targets
for
synthetic
chemistry,
and
many
methods
involving
the
aziridination
of
alkenes
by
olefins
with
nitrenes
have
been
reported.
In
general,
however,
nitrene
transfer
reactions
optimized
a
limited
range
precursors,
synthesis
structurally
diverse
aziridines
featuring
N-substituents
requires
application
multiple
varying
reaction
conditions.
Herein,
we
report
photocatalytic
method
that
operates
wide
N-substituted
precursors.
A
combination
synthetic,
spectroscopic,
computational
data
is
consistent
mechanism
generation
triplet
intermediates.
The
effectiveness
4DPAIPN
as
photocatalyst
this
process
can
be
rationalized
consequence
its
exceptionally
long
lifetime,
rather
than
excited
state
energies
or
redox
properties
in
isolation.
Dalton Transactions,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Jan. 1, 2025
Compared
to
aziridines,
azaphosphiridines,
which
formally
result
from
the
replacement
of
a
carbon
atom
by
phosphorus,
have
been
much
less
studied.
In
this
work,
accurate
values
for
one
most
prominent
properties,
ring
strain
energy
(RSE),
theoretically
examined
wide
range
azaphosphiridine
derivatives.
Strongly
related
aspects
interest
developing
use
azaphosphiridines
in
heteroatom
and
polymer
chemistry
are
opening
reactions
polymerisations,
latter
facilitated
their
significantly
high
RSE.
While
methyl
groups
little
influence
on
RSE,
complexation
with
different
metal
moieties
increases
RSE
all
cases,
an
increase
was
also
found
upon
oxidation
corresponding
P-oxides
other
σ5λ5-P
The
highest
P-protonated
azaphosphiridinium
cation
exocyclic
double
bonds.
A
correlation
RSEs
relaxed
force
constants
endocyclic
bonds
AIM-derived
parameters
critical
points,
such
as
electron
density,
ρ(r),
Lagrangian
kinetic
energy,
G(r),
found.
relatively
low
barrier
P-C
bond
cleavage
via
nucleophilic
attack
MeNH2
phosphorus
points
possibility
ring-opening
polymerisation.
Pharmaceuticals,
Journal Year:
2025,
Volume and Issue:
18(3), P. 304 - 304
Published: Feb. 22, 2025
Background/Objectives:
Psoriasis,
a
prevalent
dermatological
disorder,
poses
therapeutic
challenges
due
to
limited
effective
treatments
or
adverse
side-effects.
Traditional
medicinal
plants
like
Alstonia
scholaris
and
Wrightia
tinctoria,
historically
used
in
Ayurvedic
Siddha
practices,
show
potential
treating
inflammatory
skin
diseases.
This
study
aims
explore
their
vitro
vivo
anti-psoriatic
properties
develop
safer
more
therapies.
Methods:
Chloroform:methanol
fractions
from
ethanol
extracts
of
tinctoria
were
evaluated
for
activity.
In
assays
using
HaCaT
cells
assessed
cell
viability,
apoptosis,
markers.
studies
utilized
an
IMQ-induced
psoriasis
mouse
model,
evaluating
lesions,
histopathology,
cytokine
profiles.
Results:
Chloroform
significantly
reduced
viability
induced
apoptosis.
They
also
dose-dependently
downregulated
IL-8
RANTES
levels.
vivo,
these
inflammation,
edema,
scores.
Histopathological
analysis
showed
decreased
epidermal
thickness
dermal
inflammation.
Key
biomarkers
IL-17
IL-23
reduced.
Conclusions:
demonstrated
potent
effects
vivo.
These
findings
support
as
novel
phytotherapeutic
agents
managing
psoriasis,
offering
promise
further
development
clinical
application.
