ACS Catalysis,
Journal Year:
2024,
Volume and Issue:
14(9), P. 6513 - 6524
Published: April 13, 2024
Efficient
synthesis
of
sulfonamides
has
long
been
pursued
by
chemists
due
to
their
frequent
occurrence
in
pharmaceuticals,
especially
anti-inflammatory
medicines.
The
traditional
assembly
from
sulfonyl
chlorides
and
amines,
as
well
the
recently
developed
one-step
involving
sulfur
dioxide,
still
faces
challenges
such
poor
substrate
compatibility
and/or
stringent
reaction
conditions.
Herein,
we
present
a
strategy
for
situ
generation
sulfamoyl
radicals
modular
both
alkenyl
alkyl
with
wide
applicability
(>100
examples),
mild
conditions,
easily
accessible
starting
materials.
This
method
is
successfully
applied
late-stage
modification
drug
molecules
(23
molecule
naratriptan,
15N-labeling
sulfonamides.
Chemical Science,
Journal Year:
2024,
Volume and Issue:
15(11), P. 3879 - 3892
Published: Jan. 1, 2024
The
Accelerated
SuFEx
Click
Chemistry
(ASCC)
protocol,
adapted
to
a
96-well
plate
format,
has
been
applied
the
late-stage
derivatization
of
bioactive
molecules
and
array
synthesis
anticancer
agents,
showcasing
its
potential
for
drug
discovery.
Organic Letters,
Journal Year:
2023,
Volume and Issue:
25(48), P. 8722 - 8726
Published: Nov. 29, 2023
A
photochemical
halogen-atom
transfer
(XAT)
method
for
generating
sulfonyl
radicals
from
aryl
fluorides
has
been
developed.
It
allows
the
hydrosulfonylation
of
unactivated
alkenes,
which
was
challenging
to
achieve
through
our
previous
single-electron
route.
This
reaction
excellent
functional
group
tolerance
and
substrate
scope
under
mild
conditions.
ACS Chemical Biology,
Journal Year:
2023,
Volume and Issue:
18(12), P. 2464 - 2473
Published: Nov. 21, 2023
Molecular
glue
degraders
(MGDs)
are
small
molecules
that
degrade
proteins
of
interest
via
the
ubiquitin–proteasome
system.
While
MGDs
were
historically
discovered
serendipitously,
approaches
for
MGD
discovery
now
include
cell-viability-based
drug
screens
or
data
mining
public
transcriptomics
and
response
datasets.
These
approaches,
however,
have
target
spaces
restricted
to
essential
proteins.
Here
we
develop
a
high-throughput
workflow
also
reaches
nonessential
proteome.
This
begins
with
rapid
synthesis
compound
library
by
sulfur(VI)
fluoride
exchange
chemistry
coupled
morphological
profiling
assay
in
isogenic
cell
lines
vary
levels
E3
ligase
CRBN.
By
comparing
changes
induced
treatment
across
lines,
able
identify
FL2-14
as
CRBN-dependent
targeting
protein
GSPT2.
We
envision
this
would
contribute
characterization
wider
range
ACS Catalysis,
Journal Year:
2024,
Volume and Issue:
14(9), P. 6513 - 6524
Published: April 13, 2024
Efficient
synthesis
of
sulfonamides
has
long
been
pursued
by
chemists
due
to
their
frequent
occurrence
in
pharmaceuticals,
especially
anti-inflammatory
medicines.
The
traditional
assembly
from
sulfonyl
chlorides
and
amines,
as
well
the
recently
developed
one-step
involving
sulfur
dioxide,
still
faces
challenges
such
poor
substrate
compatibility
and/or
stringent
reaction
conditions.
Herein,
we
present
a
strategy
for
situ
generation
sulfamoyl
radicals
modular
both
alkenyl
alkyl
with
wide
applicability
(>100
examples),
mild
conditions,
easily
accessible
starting
materials.
This
method
is
successfully
applied
late-stage
modification
drug
molecules
(23
molecule
naratriptan,
15N-labeling
sulfonamides.
