ChemMedChem,
Journal Year:
2022,
Volume and Issue:
18(5)
Published: Dec. 31, 2022
Innovations
in
synthetic
chemistry
have
a
profound
impact
on
the
drug
discovery
process,
and
will
always
be
necessary
driver
of
development.
As
result,
it
is
significance
to
develop
novel
simple
effective
installation
medicinal
modules
promote
discovery.
Herein,
we
developed
NaClO-mediated
cross
indoles
azoles,
both
which
are
frequently
encountered
drugs
natural
products.
This
toolbox
provides
convenient
route
access
library
N-linked
2-(azol-1-yl)
indole
derivatives,
can
used
for
late-stage
modification
drugs,
products
peptides.
Moreover,
biological
screening
has
revealed
that
several
adducts
showed
promising
anticancer
activities
against
A549
NCI-H1975
cells,
give
us
hit
The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
89(14), P. 10272 - 10282
Published: July 5, 2024
The
exploration
of
remote
functionalization
indoles
is
impeded
by
the
inherently
dominant
reactivity
intrinsic
to
pyrrole
moiety.
Herein,
we
delineate
a
novel
strategy
facilitated
Lewis
acid
mediation,
enabling
C-H
functionalization,
which
culminates
in
synthesis
an
array
selectively
functionalized
indole
derivatives,
encompassing
3-trifluoroacetyl
and
5-benzoyl
motifs,
utilizing
trifluoroacetic
anhydride
various
acyl
chlorides.
Notably,
protocol
exhibits
versatility,
as
epitomized
extension
C5-acylation
alkylation
sulfonation
reactions.
This
methodology
distinguished
its
exemplary
regio-
chemo-selectivity,
extensive
substrate
scope,
commendable
tolerance
diverse
functional
groups,
employment
comparatively
mild
reaction
conditions.
Advanced Synthesis & Catalysis,
Journal Year:
2023,
Volume and Issue:
365(7), P. 990 - 996
Published: March 14, 2023
Abstract
The
position‐selective
functionalization
of
the
poorly
reactive
benzenoid
nucleus
indoles
has
remained
a
great
challenge
in
organic
chemistry.
Here
we
describe
directing‐group‐free,
three‐component
tandem
C3‐acylation/C5,6‐H
disulfenylation
via
an
iodine‐,
Lewis
acid‐
and
Brønsted
acid‐cooperated
mediated
strategy.
This
protocol
is
remarkable
for
its
exceptional
regio‐
chemo‐selectivity,
broad
substrate
scope,
good
functional
group
tolerance
mild
reaction
conditions.
Advantageously,
present
offers
potential
development
general
site‐selective
at
indoles,
removing
requirement
neighbouring
activating
groups.
magnified
image
Organic Chemistry Frontiers,
Journal Year:
2023,
Volume and Issue:
10(23), P. 5886 - 5894
Published: Jan. 1, 2023
A
direct
C2,3–H
difunctionalization
of
indoles
with
unactivated
amines
facilitated
by
the
organo-chalconium
catalyst
generated
through
reaction
iodine
and
chalconium
reagents
has
been
developed.
Asian Journal of Organic Chemistry,
Journal Year:
2022,
Volume and Issue:
11(10)
Published: Aug. 25, 2022
Abstract
An
efficient
intermolecular
C−H
aminohalogenation
of
indoles
with
azoles
and
NXS
(X
=
F,
Cl,
Br,
I)
has
been
developed.
This
mild
protocol
provides
a
straightforward
entry
to
structurally
valuable
2‐azolyl‐3‐halogenated
in
one
single
operation.
In
addition,
this
attractive
route
for
the
synthesis
polyfunctionalized
is
great
significance
due
product's
versatile
reactivity
further
transformations.
Organic Chemistry Frontiers,
Journal Year:
2023,
Volume and Issue:
11(3), P. 871 - 884
Published: Dec. 11, 2023
A
metal-free
catalytic
method
for
the
regioselective
direct
dehydrogenation–dichalcogenation
of
indolines.
The
reaction
mechanism
and
regioselectivity
have
been
elucidated
via
density
functional
theory
studies.
ChemMedChem,
Journal Year:
2022,
Volume and Issue:
18(5)
Published: Dec. 31, 2022
Innovations
in
synthetic
chemistry
have
a
profound
impact
on
the
drug
discovery
process,
and
will
always
be
necessary
driver
of
development.
As
result,
it
is
significance
to
develop
novel
simple
effective
installation
medicinal
modules
promote
discovery.
Herein,
we
developed
NaClO-mediated
cross
indoles
azoles,
both
which
are
frequently
encountered
drugs
natural
products.
This
toolbox
provides
convenient
route
access
library
N-linked
2-(azol-1-yl)
indole
derivatives,
can
used
for
late-stage
modification
drugs,
products
peptides.
Moreover,
biological
screening
has
revealed
that
several
adducts
showed
promising
anticancer
activities
against
A549
NCI-H1975
cells,
give
us
hit
