Chemistry - Methods,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Dec. 20, 2024
Abstract
The
increased
demand
for
the
synthesis
of
Csp
3
enriched
motifs
and
urgency
discovering
new
drugs
requires
development
more
efficient
technologies
synthetic
tools
to
accelerate
drug
discovery
processes.
Herein,
we
report
a
fully
automated
strategy
addition
building
blocks
onto
olefins
via
Giese
forge
−Csp
bonds.
developed
protocol
allowed
in‐situ
conversion
aldehydes
(non‐redox‐active
species)
electroactive
imidazolidines
their
use
as
precursors
C‐centered
radicals
under
photoredox
catalyzed
conditions
bioactive
compound
libraries
by
synthesizing
sp
‐enriched
compounds.
Chemical Science,
Journal Year:
2024,
Volume and Issue:
15(36), P. 14548 - 14555
Published: Jan. 1, 2024
The
fluctuating
reproducibility
of
scientific
reports
presents
a
well-recognised
issue,
frequently
stemming
from
insufficient
standardisation,
transparency
and
lack
information
in
publications.
Angewandte Chemie International Edition,
Journal Year:
2024,
Volume and Issue:
64(1)
Published: Oct. 9, 2024
Abstract
Etherification
and
amination
of
aryl
halide
scaffolds
are
commonly
used
reactions
in
parallel
medicinal
chemistry
to
rapidly
scan
structure–activity
relationships
with
abundant
building
blocks.
Electrochemical
methods
for
etherification
demonstrate
broad
functional
group
tolerance
extended
nucleophile
scope
compared
traditional
methods.
Nevertheless,
there
is
a
need
robust
scale‐transferable
workflows
electrochemical
compound
library
synthesis.
Herein
we
describe
platform
automated
synthesis
C−X
arylation
(X=NH,
OH)
flow
access
libraries.
A
comprehensive
Design
Experiment
(DoE)
study
identifies
an
optimal
protocol
which
generates
high
yields
across>30
scaffolds,
diverse
amines
(including
electron‐deficient
sulfonamides,
sulfoximines,
amides,
anilines)
alcohols
serine
residues
within
peptides).
Reaction
sequences
on
commercially
available
equipment
generate
libraries
anilines
ethers.
The
unprecedented
application
potentiostatic
alternating
polarity
essential
avoid
accumulating
electrode
passivation.
Moreover,
it
enables
be
performed
air,
without
supporting
electrolyte
reproducibility
over
consecutive
runs.
Our
method
represents
powerful
means
independent
using
electrochemistry.
Advanced Optical Materials,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Feb. 27, 2025
Abstract
Photons
are
widely
used
for
producing
and
degrading
matter,
yet
current
approaches
their
delivery
to
unstirred
light‐absorbing
media
give
poor
uniformity
energetic
efficiency.
Here,
a
cheap
modular
Do‐It‐Yourself
(DIY)‐realizable
mini‐photoreactor
is
introduced
that
addresses
these
issues,
additionally
allows
in
situ
absorption,
fluorescence,
Nuclear
Magnetic
Resonance
(NMR)
spectroscopy.
Its
first
configuration
features
an
internal
light‐scattering
cylindrical
liquid‐filled
waveguide
scatter
light
outward
into
the
medium,
while
its
second
configuration,
meant
more
strongly
absorbing
media,
adds
external
coaxial
envelope,
allowing
balanced
injection
from
both
sides
of
medium.
Extensive
NMR‐
fluorescence‐based
characterizations
with
new
actinometers,
together
optical
simulations,
performed;
latter
key
factors
govern
photon
flux
density
distribution
be
unraveled.
The
insights
go
beyond
reactor
design,
have
relevance
analytical
photochemistry
photocatalysis,
where
characterization
widespread.
Journal of the American Chemical Society,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 21, 2025
Herein,
we
present
a
novel
class
of
diazo
compounds
as
atomic
carbon
reagents
substituted
with
two
orthogonal
redox-active
leaving
groups
that
were
exploited
in
the
late-stage
construction
chiral
centers
aryl
C–H
bonds
from
aromatic
feedstocks
and
drug
molecules.
Key
to
strategy
was
use
photoredox
catalysis
enable
an
initial
diazomethylation
reaction
able
generate
diazomethyl-substituted
esters.
Subsequent
readily
available
starting
materials
proceeded
using
broad
range
well-known
ester
functionalizations.
Moreover,
applicability
our
reagent
tested
automated
parallel
synthesis
library
Fenofibrate
derivatives.
RSC Advances,
Journal Year:
2025,
Volume and Issue:
15(19), P. 15155 - 15163
Published: Jan. 1, 2025
Herein,
a
visible
light-promoted
metal-free
protocol
for
the
synthesis
of
nitrocyclopropanes
is
reported,
exploiting
photochemical
activity
ternary
EDA
complex.
