Standardized Approach for Diversification of Complex Small Molecules via Aryl Thianthrenium Salts
Journal of the American Chemical Society,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 21, 2025
Thianthrenation
is
a
useful
strategy
for
the
late-stage
diversification
of
complex
small
molecules
owing
to
positional
selectivity
and
synthetic
versatility
thianthrenium
salts
as
electrophilic
linchpins.
However,
substrate-dependent
identification
suitable
reaction
conditions
thianthrenation
can
be
difficult.
Reported
functionalization
vary
significantly
and,
in
some
instances,
lack
robustness
practicality.
Herein,
we
report
generalized
approach
preparation
two
manifolds
practical,
robust,
parallel
salts.
Язык: Английский
Precise synthesis of ortho-deuterated aromatic derivatives: an arylthianthrenium salt-based platform approach
Chinese Chemical Letters,
Год журнала:
2025,
Номер
unknown, С. 111132 - 111132
Опубликована: Март 1, 2025
Язык: Английский
Organosilicon Precursors for Efficient Aromatic Copper-Mediated Radiocyanation
Опубликована: Июнь 26, 2024
Copper-mediated
radiolabelling
has
revolutionised
how
(hetero)aromatic
imaging
agents
are
prepared
for
positron
emission
tomography
(PET).
Despite
advancements,
this
radiochemistry
fails
to
address
critical
stability,
reactivity,
and
toxicity
concerns
encountered
in
many
labelling
systems,
which
paramount
safely
reproducibly
generating
patient
radiomedicines.
To
overcome
these
limitations,
a
copper-mediated
11C-cyanation
reaction
is
presented
that
leverages
heptamethyltrisiloxanes
as
(hetero)aryl
nucleophiles.
Rapid
ipso-radiocyanation
occurs
conversions
surpass
related
precursors
while
offering
stability
advantages.
Preliminary
mechanistic
data
suggests
difluoro(methyl)aryl
silane
may
be
generated
prior
transmetallation.
Multiple
bioactive
scaffolds
relevant
(pre)clinical
PET
were
labelled
showcase
the
broader
significance
of
protocol,
including
an
automated
radiosynthesis
-opioid
receptor
antagonist
currently
under
clinical
investigation.
Overall,
adopting
aryl
will
augment
radiochemical
space
support
production
nuclear
medicines.
Язык: Английский
C–H Labeling with [18F]Fluoride: An Emerging Methodology in Radiochemistry
ACS Central Science,
Год журнала:
2024,
Номер
10(9), С. 1674 - 1688
Опубликована: Авг. 23, 2024
Fluorine-18
is
the
most
routinely
employed
radioisotope
for
positron
emission
tomography,
a
dynamic
nuclear
imaging
modality.
The
radiolabeling
of
C–H
bonds
an
attractive
method
installing
fluorine-18
into
organic
molecules
since
it
can
preclude
cumbersome
prefunctionalization
requisite
precursors.
Although
electrophilic
"F+"
reagents
(e.g.,
[18F]F2)
are
effective
radiolabeling,
state-of-the-art
methodologies
predominantly
leverage
high
molar
activity
nucleophilic
[18F]fluoride
sources
[18F]KF)
with
substantial
(pre)clinical
advantages.
Reflecting
this,
multiple
techniques
utility
have
been
disclosed
over
past
decade.
However,
adoption
has
slow,
and
PET
agents
still
prepared
via
methods
that,
despite
level
practicality,
limited
in
scope
SNAr,
SN2
radiofluorinations).
By
addressing
drawbacks
inherent
to
these
strategies,
radiofluorination
radiofluoroalkylation
carry
potential
complement
supersede
labeling
methods,
facilitating
expedited
production
used
disease
staging
drug
development.
In
this
Outlook,
we
showcase
recent
developments
discuss
merits,
potential,
barriers
settings.
addition,
highlight
trends,
challenges,
directions
emerging
field
study.
Язык: Английский