Chemical Science,
Journal Year:
2024,
Volume and Issue:
15(28), P. 10918 - 10925
Published: Jan. 1, 2024
The
organophotocatalysed-generation
of
α-amino
radicals
enables
the
synthesis
bicyclo[n.1.1]alkanes
(
n
=
1,
3)
under
mild
conditions
by
addition
to
interbridgehead
C–C
bonds
[n.1.1]propellanes.
Chemical Society Reviews,
Journal Year:
2024,
Volume and Issue:
53(3), P. 1068 - 1089
Published: Jan. 1, 2024
Leveraging
light
energy
to
expose
the
‘dark’
reactive
states
describes
whole
essence
of
triplet–triplet
transfer.
This
offers
an
impressive
opportunity
conduct
a
multitude
diverse
reactions
and
access
sought-after
molecular
motifs.
Journal of Medicinal Chemistry,
Journal Year:
2023,
Volume and Issue:
66(18), P. 12697 - 12709
Published: Sept. 7, 2023
The
oxetane
ring
is
an
emergent,
underexplored
motif
in
drug
discovery
that
shows
attractive
properties
such
as
low
molecular
weight,
high
polarity,
and
marked
three-dimensionality.
Oxetanes
have
garnered
further
interest
isosteres
of
carbonyl
groups
tools
to
fine-tune
physicochemical
compounds
pKa,
LogD,
aqueous
solubility,
metabolic
clearance.
This
perspective
highlights
recent
applications
motifs
campaigns
(2017–2022),
with
emphasis
on
the
effect
medicinally
relevant
building
blocks
used
incorporate
ring.
Based
this
analysis,
we
provide
overview
potential
benefits
appending
a
compound,
well
pitfalls,
challenges,
future
directions.
Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
67(10), P. 7788 - 7824
Published: May 3, 2024
Triazole
demonstrates
distinctive
physicochemical
properties,
characterized
by
weak
basicity,
various
dipole
moments,
and
significant
dual
hydrogen
bond
acceptor
donor
capabilities.
These
features
are
poised
to
play
a
pivotal
role
in
drug–target
interactions.
The
inherent
polarity
of
triazole
contributes
its
lower
logP,
suggesting
the
potential
improvement
water
solubility.
metabolic
stability
adds
additional
value
drug
discovery.
Moreover,
metal-binding
capacity
nitrogen
atom
lone
pair
electrons
has
broad
applications
development
metal
chelators
antifungal
agents.
This
Perspective
aims
underscore
unique
attributes
application.
A
comparative
analysis
involving
isomers
other
heterocycles
provides
guiding
insights
for
subsequent
design
triazoles,
with
hope
offering
valuable
considerations
designing
medicinal
chemistry.
Journal of the American Chemical Society,
Journal Year:
2024,
Volume and Issue:
146(8), P. 5067 - 5073
Published: Feb. 16, 2024
The
replacement
of
a
functional
group
with
its
corresponding
bioisostere
is
widely
employed
tactic
during
drug
discovery
campaigns
that
allows
medicinal
chemists
to
improve
the
ADME
properties
candidates
while
maintaining
potency.
However,
incorporation
bioisosteres
typically
requires
lengthy
de
novo
resynthesis
potential
candidates,
which
represents
bottleneck
in
their
broader
evaluation.
An
alternative
would
be
directly
convert
into
at
late
stage.
Herein,
we
report
realization
this
approach
through
conversion
aliphatic
alcohols
difluoromethylated
analogues
via
merger
benzoxazolium-mediated
deoxygenation
and
copper-mediated
C(sp3)–CF2H
bond
formation.
utility
method
showcased
variety
complex
compounds.
Journal of the American Chemical Society,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Sept. 25, 2024
The
selective
construction
of
bridged
bicyclic
scaffolds
has
garnered
increasing
attention
because
their
extensive
use
as
saturated
bioisosteres
arene
in
pharmaceutical
industry.
However,
sharp
contrast
to
racemic
counterparts,
assembling
chiral
structures
an
enantioselective
and
regioselective
manner
remains
challenging.
Herein,
we
describe
our
protocol
for
constructing
2-oxa-3-azabicyclo[3.1.1]heptanes
(BCHeps)
by
[4π
+
2σ]
cycloadditions
bicyclo[1.1.0]butanes
(BCBs)
nitrones
taking
advantage
a
copper(II)
complex
Lewis
acid
catalyst.
This
method
features
mild
conditions,
good
functional
group
tolerance,
high
yield
(up
99%),
excellent
enantioselectivity
99%
ee).
Density
theory
(DFT)
calculation
elucidates
the
origin
reaction's
mechanism
BCB
activation
Cu(II)
complex.
Organic Letters,
Journal Year:
2024,
Volume and Issue:
26(3), P. 713 - 718
Published: Jan. 12, 2024
Sulfonamides
are
important
structures
in
pharmaceuticals,
agrochemicals,
and
organocatalysts,
yet
the
rapid
benign
synthesis
of
these
compounds
is
still
a
great
challenge.
Herein
we
report
photoinduced
method
for
synthesizing
sulfonamides
from
(hetero)aryl
carboxylic
acid
oxime
esters.
This
reaction
proceeds
via
one-pot
cascade
radical–radical
cross-coupling
by
energy-transfer-mediated
photocatalysis.
A
wide
substrate
scope
including
substrates
late-stage
modification
pharmaceutical
molecular
entities
reveal
its
generality.
Nature Communications,
Journal Year:
2024,
Volume and Issue:
15(1)
Published: April 18, 2024
Catalysed
C-H
activation
has
emerged
as
a
transformative
platform
for
molecular
synthesis
and
provides
new
opportunities
in
drug
discovery
by
late-stage
functionalisation
(LSF)
of
complex
molecules.
Notably,
small
aliphatic
motifs
have
gained
significant
interest
medicinal
chemistry
their
beneficial
properties
applications
sp
International Journal of Molecular Sciences,
Journal Year:
2024,
Volume and Issue:
25(23), P. 13121 - 13121
Published: Dec. 6, 2024
The
bioavailability
of
small-molecule
drugs
remains
a
critical
challenge
in
pharmaceutical
development,
significantly
impacting
therapeutic
efficacy
and
commercial
viability.
This
review
synthesizes
recent
advances
understanding
overcoming
limitations,
focusing
on
key
physicochemical
biological
factors
influencing
drug
absorption
distribution.
We
examine
cutting-edge
strategies
for
enhancing
bioavailability,
including
innovative
formulation
approaches,
rational
structural
modifications,
the
application
artificial
intelligence
design.
integration
nanotechnology,
3D
printing,
stimuli-responsive
delivery
systems
are
highlighted
as
promising
avenues
improving
delivery.
discuss
importance
holistic,
multidisciplinary
approach
to
optimization,
emphasizing
early-stage
consideration
ADME
properties
need
patient-centric
also
explores
emerging
technologies
such
CRISPR-Cas9-mediated
personalization
microbiome
modulation
tailored
enhancement.
Finally,
we
outline
future
research
directions,
advanced
predictive
modeling,
barriers,
addressing
challenges
modalities.
By
elucidating
complex
interplay
affecting
this
aims
guide
efforts
developing
more
effective
accessible
therapeutics.