Handbook of CH‐Functionalization,
Journal Year:
2022,
Volume and Issue:
unknown, P. 1 - 147
Published: Oct. 2, 2022
Abstract
Tremendous
advances
in
transition
metal‐catalyzed
CH
functionalization
of
the
indole
scaffolds
have
been
recently
reported.
Great
efforts
devoted
to
directing
group
strategy
development
selectivity
achievement
overriding
both
inherent
reactivity
scaffold
and
activation
C2/C3H
bonds.
This
article
aims
highlight
elegant
methods
enabling
direct
arylation,
alkenylation,
alkylation,
alkynylation
along
with
introduction
heteroatoms
into
via
selective
strategies.
Organic Chemistry Frontiers,
Journal Year:
2021,
Volume and Issue:
8(14), P. 3809 - 3814
Published: Jan. 1, 2021
An
efficient
regioselective
and
stereoselective
cascade
annulation
of
indoles
with
alkynediones
has
been
developed
for
construction
free
(NH)
tetrahydrocarbazoles
continuous
quaternary
carbons
via
Cp*RhIII-catalyzed
indole
C2–H
activation.
Frontiers in Cellular and Infection Microbiology,
Journal Year:
2022,
Volume and Issue:
12
Published: Oct. 13, 2022
Multi-drug
resistant
Staphylococcus
aureus
infection
is
still
a
serious
threat
to
global
health.
Therefore,
there
an
urgent
need
develop
new
antibacterial
agents
based
on
virulence
factor
therapy
overcome
drug
resistance.
Previously,
we
synthesized
SYG-180-2-2
(C
21
H
16
N
2
OSe),
effective
small
molecule
compound
against
biofilm.
The
aim
of
this
study
was
investigate
the
anti-virulence
efficacy
.
MIC
results
demonstrated
no
apparent
activity
SYG-180-2-2.
growth
curve
assay
showed
that
had
nonlethal
effect
S.
Besides,
strongly
inhibited
hemolytic
and
staphyloxanthin
synthesis
in
Inhibition
by
enhanced
sensitivity
oxidants
human
whole
blood.
In
addition,
significantly
decreased
expression
saeR
-mediated
gene
hlb
staphyloxanthin-related
crtM
,
crtN
sigB
genes
quantitative
polymerase
chain
reaction
(qPCR).
Meanwhile,
oxidative
stress-related
sodA
sodM
katA
also
decreased.
Galleria
Mellonella
revealed
not
toxic
larvae.
Further,
larvae
model
bacteria
reduced
after
4
μg/mL
treatment.
skin
abscess
formation
mice
reducing
bacterial
burden
subcutaneous
inflammation.
conclusion,
might
be
promising
agent
attenuate
targeting
associated
with
synthesis.
The Journal of Organic Chemistry,
Journal Year:
2022,
Volume and Issue:
87(9), P. 5543 - 5555
Published: April 13, 2022
Using
N-methoxyamide
reagents
as
an
amide
source,
C–H
amidation
was
realized
at
the
ortho
position
of
azine
under
action
rhodium
and
boric
acid.
The
method
has
mild
reaction
conditions,
high
atomic
utilization,
excellent
yield,
wide
adaptability
to
(both
aromatic
amides
fatty
are
applicable).
Amide-substituted
ketones
can
be
obtained
by
a
simple
treatment
further
transformed
into
bioactive
substances.
This
provides
good
supplement
for
bond
rings.
Advanced Synthesis & Catalysis,
Journal Year:
2023,
Volume and Issue:
365(24), P. 4495 - 4501
Published: Sept. 18, 2023
Abstract
Dioxazolones
and
phosphines
have
been
used
to
access
N
‐acyl
iminophosphoranes
in
copper(I)
catalysis
under
simple
thermal
conditions.
The
synthetic
utility
of
this
protocol
is
demonstrated
by
a
broad
range
substrates
with
an
excellent
atom‐economy.
optimization
process
showed
that
copper
as
catalytic
amount
toward
the
targeted
transformation.
Functionalization
studies
were
also
conducted.
Our
reaction
compatible
example
bioactive
motif‐containing
iminophosphorane
analogue.
Organic Letters,
Journal Year:
2022,
Volume and Issue:
24(14), P. 2665 - 2669
Published: April 4, 2022
A
process
for
the
synthesis
of
C7-functionalized
indoles
using
para-substituted
2-alkynylanilines
as
starting
materials
was
reported.
The
involves
a
dearomatization,
an
1,2-addition
by
organic
lithium
or
Grignard
reagents,
aromatization-driven
allylic
rearrangement,
and
cyclization.
variety
groups
including
alkyl,
aryl,
alkenyl,
alkynyl
were
selectively
installed
at
C7
site
leading
to
formation
2,5,7-trisubstituted
indoles.
Israel Journal of Chemistry,
Journal Year:
2023,
Volume and Issue:
64(1-2)
Published: Sept. 25, 2023
Abstract
Indole
derivatives
are
fundamental
structural
units
in
many
bioactive
compounds
and
molecular
materials.
The
site‐selective
C7‐functionalization
of
these
moieties
has
been
proven
to
be
extremely
challenging
due
the
inherent
reactivity
C2‐
C3‐positions.
Herein,
we
report
first
electro‐C7‐alkenylation
indoles.
This
novel
sustainable
methodology
provides
highly
exclusive
access
C7‐position
devoid
often
toxic
expensive
chemical
oxidants.
Moreover,
an
array
substrates
was
successfully
alkenylated
at
C7‐position,
versatile
product
diversification
achieved.
Organic Letters,
Journal Year:
2024,
Volume and Issue:
26(38), P. 8051 - 8056
Published: Sept. 16, 2024
A
Ru(II)-catalyzed
skeletal
editing
of
oxindole
scaffolds
was
established
to
afford
C7-alkyl
acetate
indole
derivatives
using
internal
alkyne
and
alkyl
alcohol.
The
developed
method
is
simple,
efficient,
straightforward.
reaction
extended
substrates
having
wide
chemoselective
profiles.
When
unsymmetrical
alkynes
were
used,
promising
regioselectivity
realized.
preliminary
mechanistic
study
revealed
that
the
pathway
proceeded
by
Ru(II)/Ag(I)-catalyzed
amide
cleavage
subsequent
oxidative
annulation.
Chemistry - An Asian Journal,
Journal Year:
2023,
Volume and Issue:
18(14)
Published: June 10, 2023
A
direct
protocol
for
Rh-catalyzed
C-H
amidation
of
ferrocenes
in
a
ball
mill
using
dioxazolones
as
the
amide
source
under
solvent-free
conditions
was
developed.
The
corresponding
ortho-aminated
products
were
formed
3
hours
and
yields
up
to
99%
absence
base.
This
method
could
be
typically
sustainable
environmental-friendly
alternative
traditional
methodologies,
with
advantages
wide
substrate
range,
good
functional
group
tolerance
gram-scale
synthesis.
