The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
89(7), P. 5010 - 5018
Published: March 27, 2024
Recent
years
have
seen
novel
modalities
emerge
for
the
treatment
of
human
diseases
resulting
in
an
increase
beyond
rule
5
(bRo5)
chemical
matter.
As
a
result,
synthetic
innovations
aiming
to
enable
rapid
access
complex
bRo5
molecular
entities
become
increasingly
valuable
medicinal
chemists'
toolkits.
Herein,
we
report
general
synthesis
new
class
noncanonical
amino
acids
(ncAA)
with
cyclopropyl
backbone
achieve
conformational
constraint
and
bearing
C(sp3)-rich
benzene
bioisosteres.
We
also
demonstrate
preliminary
studies
toward
utilities
these
ncAA
as
building
blocks
chemistry
research.
Chinese Journal of Chemistry,
Journal Year:
2024,
Volume and Issue:
42(13), P. 1509 - 1514
Published: March 7, 2024
Comprehensive
Summary
The
first
total
synthesis
of
talaroconvolutin
A
(1.1
g
obtained)
and
talarofuranone
has
been
achieved
using
accessible
materials
(12
steps,
7.5%
8.2%
yields,
respectively).
Convergent
routes
involved
intramolecular
Diels−Alder
reactions
in
two
approaches
for
creating
the
decalin
moiety.
Additionally,
an
unprecedented
DMP‐mediated
domino
reaction
resulted
deoxy‐tetramic
acid
system.
These
syntheses
not
only
establish
absolute
configuration
but
also
enable
further
collaborative
studies
this
type
ferroptosis
inducers.
European Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
27(40)
Published: Aug. 9, 2024
Abstract
A
palladium
catalyst
supported
on
silk
fibroin
(Pd/SF)
has
been
tested
in
the
Sonogashira
coupling
reactions
of
a
wide
range
aryl
iodides
and
terminal
alkynes.
The
best
catalytic
performance
was
obtained
at
90
°C
using
only
0.25
mol
%
metal
loading
under
copper‐free
conditions,
presence
H
2
O/EtOH
(3
:
v/v)
solvent
mixture
triethylamine
as
base,
affording
products
good
yields.
Pd/SF‐based
protocol
then
successfully
extended
to
synthesis
benzofurans
through
Sonogashira‐Cacchi
type
annulation
2‐iodophenol
with
Preliminary
investigations
recyclability
heterogeneous
behaviour
were
performed:
hot
filtration
test
leaching
evidenced
small
amount
soluble
active
species
into
reaction
mixture.
Nevertheless,
Pd/SF
could
be
reused
recharging
it
can
recycled
four
consecutive
runs
no
significant
deactivation.
Applied Organometallic Chemistry,
Journal Year:
2024,
Volume and Issue:
39(1)
Published: Dec. 17, 2024
ABSTRACT
Metal‐catalyzed
cross‐coupling
reactions
are
essential
tools
for
constructing
C–C
bonds
in
organic
synthesis.
Among
these
prominent
approaches,
the
Sonogashira
reaction
stands
out
as
a
key
player
and
is
widely
utilized
medicinal
chemistry.
This
versatile
method
enables
creation
of
complex
C
(sp
2
)–C
(sp)
by
linking
aryl
or
vinyl
halides
with
terminal
alkynes,
facilitating
efficient
construction
molecular
structures
crucial
drug
development.
A
notable
application
its
ability
to
incorporate
aromatic
alkynyl
functionalities
into
pharmaceutical
compounds.
Depending
on
impactful
catalytic
system
evolved
gradually,
can
involve
either
double‐metal
catalysis
single‐metal
catalysis.
review
sheds
light
diverse
applications
coupling
approach
synthesis
generation
their
derivatives.
The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
89(7), P. 5010 - 5018
Published: March 27, 2024
Recent
years
have
seen
novel
modalities
emerge
for
the
treatment
of
human
diseases
resulting
in
an
increase
beyond
rule
5
(bRo5)
chemical
matter.
As
a
result,
synthetic
innovations
aiming
to
enable
rapid
access
complex
bRo5
molecular
entities
become
increasingly
valuable
medicinal
chemists'
toolkits.
Herein,
we
report
general
synthesis
new
class
noncanonical
amino
acids
(ncAA)
with
cyclopropyl
backbone
achieve
conformational
constraint
and
bearing
C(sp3)-rich
benzene
bioisosteres.
We
also
demonstrate
preliminary
studies
toward
utilities
these
ncAA
as
building
blocks
chemistry
research.
