Bioconjugate Chemistry,
Journal Year:
2023,
Volume and Issue:
34(8), P. 1459 - 1466
Published: July 14, 2023
The
DNA-encoded
chemical
library
(DEL)
is
a
powerful
hit
selection
technique
in
either
basic
science
or
innovative
drug
discovery.
With
the
aim
to
circumvent
issue
concerning
DNA
barcode
damage
conventional
on-DNA
copper-catalyzed
azide–alkyne
cycloaddition
reaction
(CuAAC),
we
have
successfully
developed
first
DNA-compatible
enolate–azide
[3
+
2]
reaction.
merits
of
this
DEL
chemistry
include
metal-free
and
high
fidelity,
conversions
easy
operation,
broad
substrate
scope,
ready
access
highly
substituted
1,4,5-trisubstituted
triazoles.
Thus,
it
will
not
only
further
enrich
toolbox
but
also
great
potential
practical
synthesis.
Acta Pharmaceutica Sinica B,
Journal Year:
2023,
Volume and Issue:
14(2), P. 492 - 516
Published: Oct. 11, 2023
DNA-encoded
chemical
library
(DEL)
links
the
power
of
amplifiable
genetics
and
non-self-replicating
phenotypes,
generating
a
diverse
world.
In
analogy
with
biological
world,
DEL
world
can
evolve
by
using
central
dogma,
wherein
DNA
replicates
PCR
reactions
to
amplify
genetic
codes,
sequencing
transcripts
information,
DNA-compatible
synthesis
translates
into
phenotypes.
Importantly,
is
key
expanding
space.
Besides,
evolution-driven
selection
system
pushes
chemicals
under
selective
pressure,
i.e.,
desired
strategies.
this
perspective,
we
summarized
recent
advances
in
synthetic
toolbox
panning
strategies,
which
will
shed
light
on
drug
discovery
harnessing
vitro
evolution
via
DEL.
Angewandte Chemie International Edition,
Journal Year:
2022,
Volume and Issue:
61(35)
Published: May 17, 2022
Abstract
Click
chemistry
is
a
concept
wherein
modular
synthesis
used
for
rapid
functional
discovery.
To
this
end,
continuous
discovery
of
clickable
chemical
transformations
the
pillar
to
support
development
field.
This
report
details
C3‐H
selenylation
indole
that
suitable
on‐plate
parallel
and
DNA‐encoded
library
(
Se
DEL)
via
bioinspired
LUMO
activation
strategy.
reaction
modular,
robust
highly
site‐selective,
it
features
simple
mild
system
(catalyzed
by
nonmetallic
B(C
6
F
5
)
3
at
room
temperature),
high
yields
excellent
group
compatibility.
Using
method,
1350
indole‐selenides
was
synthesized
in
an
efficient
practical
manner,
enabling
identification
ai
as
promising
compound
with
nanomolar
antiproliferative
activity
cancer
cells
situ
phenotypic
screening.
These
results
indicate
great
potential
new
high‐throughput
medicinal
biology.
Organic Chemistry Frontiers,
Journal Year:
2022,
Volume and Issue:
9(19), P. 5272 - 5280
Published: Jan. 1, 2022
A
highly
regioselective
silylation
of
unsymmetric
gem
-difluorocyclopropenes
was
achieved
by
the
capture
in-situ
formed
silyl
metal
intermediates,
which
gave
structurally
diverse
silyldifluorocyclopropanes
with
good
yields
and
stereoselectivity.
Organic Chemistry Frontiers,
Journal Year:
2022,
Volume and Issue:
9(21), P. 5976 - 5982
Published: Jan. 1, 2022
Presented
herein
is
an
efficient
and
concise
synthesis
of
fluorinated
pyridopyrimidinone
derivatives
through
formal
[3
+
3]/[5
1]
annulation
1-arylpyrazolidinones
with
gem
-difluorocyclopropenes.
Organic & Biomolecular Chemistry,
Journal Year:
2022,
Volume and Issue:
20(19), P. 3847 - 3869
Published: Jan. 1, 2022
Direct
construction
of
heterocyclic
skeletons
via
the
reactions
stable
cyclopropenes,
reactive
cyclopropenes
generated
in
situ
and
cyclopropene
precursors
is
described
with
or
without
transition
metal
catalysts.
The Journal of Organic Chemistry,
Journal Year:
2023,
Volume and Issue:
88(6), P. 3499 - 3508
Published: March 9, 2023
Rh(III)-catalyzed
C-H/N-H
annulation
and
C-H
allylation
of
phenylindazolones
have
been
realized
by
employing
5-methylene-1,3-dioxan-2-one
4-vinyl-1,3-dioxolan-2-one
as
scalable
cross-coupling
partners,
delivering
functionalized
indazolone
fused
heterocycles
branched
linear
allyl
indazolones
respectively
in
moderate
to
high
yield.
These
divergent
synthesis
protocols
showcase
mild
conditions,
broad
substrate
scope,
functional-group
compatibility.
In
addition,
scale-up
preliminary
mechanistic
exploratory
were
also
accomplished.
