Angewandte Chemie,
Journal Year:
2023,
Volume and Issue:
135(41)
Published: Aug. 21, 2023
Abstract
β‐(Hetero)arylethylamines
appear
in
a
myriad
of
pharmaceuticals
due
to
their
broad
spectrum
biological
properties,
making
them
prime
candidates
for
drug
discovery.
Conventional
methods
preparation
often
require
engineered
substrates
that
limit
the
flexibility
synthetic
routes
and
diversity
compounds
can
be
accessed.
Consequently,
provide
rapid
versatile
access
those
scaffolds
remain
limited.
To
overcome
these
challenges,
chemists
have
designed
innovative
modular
strategies
β‐(hetero)arylethylamine
motif,
paving
way
more
extensive
use
future
pharmaceuticals.
This
review
outlines
recent
progresses
synthesis
(hetero)arylethylamines
emphasizes
how
innovations
enabled
new
levels
molecular
complexity,
selectivity,
practicality.
ACS Catalysis,
Journal Year:
2025,
Volume and Issue:
15(3), P. 2139 - 2149
Published: Jan. 22, 2025
(Hetero)arylethylamines
are
privileged
substructures
in
pharmaceuticals,
agrochemicals,
and
other
bioactive
compounds.
In
principle,
the
amino–(hetero)arylation
of
olefins
represents
an
ideal
strategy
for
rapid
preparation
these
pharmacophores,
which
could
accelerate
discovery
valuable
new
products.
Established
methods,
however,
do
not
accommodate
several
important
classes
(hetero)aromatic
structures,
precludes
access
to
appreciable
range
molecular
architectures.
To
address
limitations,
we
have
developed
a
radical-mediated
reaction
that
adds
amino
(hetero)aryl
groups
from
simple
stable
sulfonamide
across
alkene.
The
identification
readily
available
triazine
as
original
N-protecting
group
was
critical
development
this
transformation.
features
good
regio-
stereoselectivity
succeeds
with
medicinally
unproductive
alternate
protocols.
Lastly,
highlighted
advances
by
synthesizing
TMP269,
class
IIa
histone
deacetylase
inhibitor
would
otherwise
be
challenging
prepare
olefin
amino–arylation.
Organic Chemistry Frontiers,
Journal Year:
2024,
Volume and Issue:
11(22), P. 6340 - 6346
Published: Jan. 1, 2024
We
developed
the
first
transition-metal-catalyzed,
regiodivergent
sulfonylation
of
aziridines,
enabling
efficient
synthesis
diverse
β-amino
sulfones
under
mild
conditions
with
broad
substrate
compatibility
and
high
regioselectivity.
Angewandte Chemie,
Journal Year:
2023,
Volume and Issue:
135(45)
Published: June 16, 2023
Abstract
Electrochemistry
utilizes
electrons
as
a
potent,
controllable,
and
traceless
alternative
to
chemical
oxidants
or
reductants,
typically
offers
more
sustainable
option
for
achieving
selective
organic
synthesis.
Recently,
the
merger
of
electrochemistry
with
readily
available
electrophiles
has
been
recognized
viable
increasingly
popular
methodology
efficiently
constructing
challenging
C−C
C‐heteroatom
bonds
in
manner
complex
molecules.
In
this
mini‐review,
we
have
systematically
summarized
most
recent
advances
electroreductive
cross‐electrophile
coupling
(eXEC)
reactions
during
last
decade.
Our
focus
on
electrophiles,
including
aryl
alkyl
(pseudo)halides,
well
small
molecules
such
CO
2
,
SO
D
O.
The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
89(16), P. 11429 - 11445
Published: Aug. 1, 2024
A
transition
metal-free,
atom-economical,
and
highly
stereospecific
synthetic
approach
to
Friedel–Crafts-type
alkylation
of
arenes/heteroarenes
has
been
developed.
The
protocol
involves
the
catalytic
aminium
radical-cation
salt
(Magic
Blue)-initiated
SN2-type
nucleophilic
ring
opening
activated
aziridines
with
give
corresponding
2,2-diarylethylamines
up
99%
yield
85%
ee
(for
nonracemic
aziridines)
in
a
very
short
reaction
time.
Moreover,
on
1,3-dimethylindole
benzofuran,
undergo
domino-ring-opening
cyclization
(DROC)
various
biologically
significant
heterocyclic
scaffolds
moderate
good
yields.
SynOpen,
Journal Year:
2024,
Volume and Issue:
08(02), P. 116 - 124
Published: April 1, 2024
Abstract
The
electrochemical
fixation
of
carbon
dioxide
onto
organic
matter
has
emerged
as
a
promising
approach
in
recent
years.
By
combining
the
unique
features
electrochemistry
with
goal
fixation,
researchers
aim
to
develop
new
strategies
that
can
contribute
more
sustainable
and
environmentally
friendly
synthesis
compounds.
One
advantage
methods
is
their
ability
provide
both
electrons
energy
for
chemical
transformations.
This
allows
direct
conversion
into
valuable
products,
without
need
transition
metal
catalysts
or
harsh
reaction
conditions.
As
result,
offers
potential
milder
efficient
processes
compared
traditional
methods.
Scientists
have
made
noteworthy
progress
exploring
different
under
These
involve
activation
various
types
bonds,
including
C(sp2)–C(sp2),
C(sp2)–H,
C–X
(X
=
halogen),
C(sp3)–X
S,
C,
O,
N).
review
aims
an
overview
current
state
research
on
matter.
It
will
discuss
employed,
key
findings,
challenges
remain
be
addressed.
highlighting
advancements
this
field,
hopes
inspire
further
exploration
innovation
area
fixation.
1
Introduction
2
Electrocatalytic
Monocarboxylation
CO2
2.1
C(sp2)–C(sp2)
2.2
C(sp2)–H
2.3
Cl,
Br,
I)
2.4
N)
3
Dicarboxylation
4
Esterification
5
Conclusions
Angewandte Chemie,
Journal Year:
2024,
Volume and Issue:
136(29)
Published: May 2, 2024
Abstract
Die
Synthese
sp
3
‐hybridsierter
kohlenstoffreicher
Moleküle
ist
aufgrund
ihrer
Bedeutung
und
ihres
Erfolgs
insbesondere
in
klinischen
Studien
von
besonderem
Interesse.
In
dieser
Arbeit
wurde
das
Einbringen
aliphatischen
Ketten
auf
ein
aromatisches
Gerüst
durch
eine
Nickel‐katalysierte
C(sp
2
)−C(sp
)
elektrophile
Kreuzkupplungen
mit
Arylsulfoniumsalzen
erreicht.
So
konnten
einfach,
nichtpräfunktionalisiere
Arene
die
Bildung
Aryldibenzothiopheniumsalze
alkyliert
werden.
Durch
den
elektrochemischen
Ansatz
können
potenziell
gefährliche
chemische
Redoxreagenzien
vermieden
Insbesondere
Ein‐Topf
Alkylierung
erwies
sich
als
praktikabel,
was
Robustheit
unseres
Ansatzes
unterstreicht.
Organic Letters,
Journal Year:
2024,
Volume and Issue:
26(30), P. 6364 - 6369
Published: July 25, 2024
Cross-electrophile
coupling
reactions
of
different
electrophiles
have
been
extensively
studied
but
mainly
limited
to
bromides
and
iodides.
Here,
we
report
an
electrochemically
induced
nickel-catalyzed
cross-electrophile
strategy
between
alkenyl
triflates
α-chloroamides
in
undivided
cell
under
mild
reaction
conditions,
affording
the
α-functionalized
amide
derivatives
good
excellent
yields
with
broad
substrate
scopes
functional
group
tolerance.
The
control
experiments
were
conducted,
a
plausible
mechanism
was
proposed.
Angewandte Chemie,
Journal Year:
2023,
Volume and Issue:
135(41)
Published: Aug. 21, 2023
Abstract
β‐(Hetero)arylethylamines
appear
in
a
myriad
of
pharmaceuticals
due
to
their
broad
spectrum
biological
properties,
making
them
prime
candidates
for
drug
discovery.
Conventional
methods
preparation
often
require
engineered
substrates
that
limit
the
flexibility
synthetic
routes
and
diversity
compounds
can
be
accessed.
Consequently,
provide
rapid
versatile
access
those
scaffolds
remain
limited.
To
overcome
these
challenges,
chemists
have
designed
innovative
modular
strategies
β‐(hetero)arylethylamine
motif,
paving
way
more
extensive
use
future
pharmaceuticals.
This
review
outlines
recent
progresses
synthesis
(hetero)arylethylamines
emphasizes
how
innovations
enabled
new
levels
molecular
complexity,
selectivity,
practicality.
