ACS Catalysis,
Год журнала:
2024,
Номер
14(9), С. 6513 - 6524
Опубликована: Апрель 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 Communications,
Год журнала:
2022,
Номер
58(67), С. 9409 - 9412
Опубликована: Янв. 1, 2022
Sulfonyl
fluorides
are
emerging
as
key
structural
motifs
in
organic
synthesis,
medicinal
chemistry,
and
materials
science.
Herein
we
report
two
efficient
complementary
methods
for
direct
decarboxylative
fluorosulfonylation
of
carboxylic
acids
by
the
merging
copper
catalysis
with
different
N-centered
HAT
regents.
A
wide
range
structurally
diverse
sulfonyl
was
readily
accessed
from
primary,
secondary,
tertiary
a
single
step
under
mild
conditions.
ACS Chemical Biology,
Год журнала:
2023,
Номер
18(12), С. 2464 - 2473
Опубликована: Ноя. 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
Chemical Science,
Год журнала:
2024,
Номер
15(11), С. 3879 - 3892
Опубликована: Янв. 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.
ACS Catalysis,
Год журнала:
2024,
Номер
14(9), С. 6513 - 6524
Опубликована: Апрель 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.
