International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(20), P. 15120 - 15120
Published: Oct. 12, 2023
Fifty-two
kinds
of
N′-phenylhydrazides
were
successfully
designed
and
synthesized.
Their
antifungal
activity
in
vitro
against
five
strains
C.
albicans
(Candida
albicans)
was
evaluated.
All
prepared
compounds
showed
varying
degrees
their
MIC80
(the
concentration
tested
when
inhibition
rate
at
80%),
TAI
(total
index),
TSI
susceptibility
index)
calculated.
The
inhibitory
activities
27/52
fluconazole-resistant
fungi
4395
5272
much
better
than
those
fluconazole.
values
14/52
fungus
5122
less
4
μg/mL,
so
it
the
most
sensitive
(TSIB
=
12.0).
A11
best
SC5314,
4395,
(MIC80
1.9,
4.0,
3.7
μg/mL).
B14
D5
four
(2.71),
(2.13),
(2.25)
are
highest.
Further
exploration
mechanisms
revealed
that
treated
with
compound
produced
free
radicals
reactive
oxygen
species,
mycelium
morphology
damaged.
In
conclusion,
N′-phenylhydrazide
scaffold
potential
development
lead
compounds.
Among
them,
A11,
B14,
demonstrated
particularly
promising
held
as
novel
agents.
Organic & Biomolecular Chemistry,
Journal Year:
2024,
Volume and Issue:
22(31), P. 6246 - 6276
Published: Jan. 1, 2024
Recent
advances
in
the
preparation
of
trifluoromethyl-containing
heterocyclics
via
trifluoromethyl
building
block
strategies
over
period
from
2019
to
present
are
systematically
summarized
and
discussed.
Organic Letters,
Journal Year:
2024,
Volume and Issue:
26(1), P. 62 - 67
Published: Jan. 3, 2024
We
have
found
a
chameleonic
reactivity
of
imidoyl
sulfoxonium
ylides.
On
the
one
hand,
ylides
react
with
electron-deficient
reagents,
such
as
alkynyl
esters,
to
lead
formation
1,2-dihydro-pyridines.
The
methyl
group
attached
sulfur
atom
acts
methylene
donor.
other
pyridinium
1,4-zwitterionic
thiolates,
which
leads
functionalized
pyrroles.
Both
transformations
feature
mild
reaction
conditions
and
good
functional
tolerance.
Organic Chemistry Frontiers,
Journal Year:
2023,
Volume and Issue:
10(15), P. 3843 - 3848
Published: Jan. 1, 2023
We
have
developed
a
Rh(
iii
)-catalyzed
C–H
activation/chemodivergent
annulation
of
N
-carbamoylindoles
with
TFISYs,
allowing
facile
access
to
variety
trifluoromethyl-substituted
(dihydro)pyrimidoindolones
high
efficiency.
Solvents
play
critical
role
in
the
selectivity
reaction.
Advanced Synthesis & Catalysis,
Journal Year:
2023,
Volume and Issue:
365(22), P. 3855 - 3860
Published: Oct. 18, 2023
Abstract
A
rhodium(III)‐catalyzed
C−H
activation/[4+1]
annulation
of
2‐aryl‐3
H
‐indoles
and
CF
3
‐substituted
imidoyl
sulfoxonium
ylides
(TFISYs)
has
been
achieved,
producing
a
wide
variety
trifluoroacetimidoyl‐substituted
11
‐isoindolo[2,1‐a]indoles
in
51–86%
yields.
The
cascade
reaction
involves
imidoylmethylation,
tautomerization
AgOAc‐mediated
C−N
bond
formation
sequence.
could
be
scaled
up
to
2
mmol
scale.
Chinese Journal of Chemistry,
Journal Year:
2023,
Volume and Issue:
41(23), P. 3205 - 3210
Published: July 17, 2023
Comprehensive
Summary
A
thermally‐induced
multi‐component
reaction
of
CF
3
‐substituted
imidoyl
sulfoxonium
ylides
(TFISYs),
amines
and
(triphenylphosphonio)difluoroacetate
(PDFA)
has
been
developed,
allowing
a
facile
access
to
2‐trifluoromethyl‐4‐aminoquinolines
in
high
yields.
The
proceeds
smoothly
with
or
without
the
addition
sulfur
utilizes
difluorocarbene
as
C1
synthon
under
simply
heating
conditions.
Mechanistic
study
reveals
that
in‐situ
generated
thiocarbonyl
fluoride,
isothiocyanate
gem
‐difluoroalkene
might
act
key
intermediates.
Organic Letters,
Journal Year:
2023,
Volume and Issue:
25(38), P. 7046 - 7050
Published: Sept. 18, 2023
A
base-mediated
cascade
reaction
of
CF3-imidoyl
sulfoxonium
ylides
and
azo
compounds
has
been
achieved,
allowing
for
facile
access
to
trifluoromethyl-substituted
1,2-dihydroquinoxalines
diimines
in
moderate
excellent
yields.
Noteworthy
is
that
the
unusual
N-N
bond
cleavage
rearrangement
are
involved
transformations.
Chemical Reviews,
Journal Year:
2025,
Volume and Issue:
unknown
Published: April 22, 2025
Fluorine
and
nitrogen
form
a
successful
partnership
in
organic
synthesis,
medicinal
chemistry,
material
sciences.
Although
fluorine-nitrogen
chemistry
has
long
rich
history,
this
field
received
increasing
interest
made
remarkable
progress
over
the
past
two
decades,
driven
by
recent
advancements
transition
metal
organocatalysis
photochemistry.
This
review,
emphasizing
contributions
from
2015
to
2023,
aims
update
state
of
art
synthesis
applications
nitrogen-based
organofluorine
functional
molecules
chemistry.
In
dedicated
sections,
we
first
focus
on
fluorine-containing
reagents
organized
according
type
groups
attached
nitrogen,
including
N-F,
N-RF,
N-SRF,
N-ORF.
review
also
covers
nitrogen-linked
building
blocks,
catalysts,
pharmaceuticals,
agrochemicals,
underlining
these
components'
broad
applicability
growing
importance
modern
The Journal of Organic Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 4, 2025
A
catalyst
and
additive-free
[2+1]
annulation
of
3-alkenyl-oxindoles
with
CF3-imidoyl
sulfoxonium
ylides
(TFISYs)
for
the
construction
spiro
3,3'-cyclopropyl
oxindoles
has
been
achieved.
cascade
intermolecular
Micheal-addition
reaction
intramolecular
nucleophilic
substitution
sequence
might
be
involved
in
transformation,
which
afforded
a
wide
range
multisubstituted
oxindole
products
high
efficiency
diastereoselectivity.
Chemical Communications,
Journal Year:
2023,
Volume and Issue:
59(83), P. 12495 - 12498
Published: Jan. 1, 2023
CF3-substituted
imidoyl
sulfoxonium
ylides
(TFISYs)
are
extraordinarily
versatile
and
powerful
synthons
for
use
in
cyclization
chemistry
that
affords
diverse
N-heterocycles.
We
first
reacted
TFISYs
as
a
two-atom
synthon
with
readily
available
azoalkenes
then
subjected
the
products
to
metal-free
formal
(4+2)
cycloaddition
chemistry.
This
protocol
features
mild
conditions
broad
substrate
scope,
is
simple
operate,
provides
highly
functionalized
trifluoromethylpyridazines
widely
found
bioactive
molecules.
