Crystal Growth & Design,
Год журнала:
2024,
Номер
25(2), С. 444 - 451
Опубликована: Дек. 25, 2024
Solid-state
synthesis
is
an
approach
to
organic
that
desirable
because
it
can
offer
minimal
or
no
solvent
waste,
high
yields,
and
relatively
low
energy
footprints.
Herein,
we
report
the
solid-state
of
a
novel
Schiff
base,
4-{(E)-[(4-methylpyridin-3-yl)imino]methyl}benzoic
acid
(4-PIBZ),
synthesized
through
reaction
amine
aldehyde.
4-PIBZ
was
prepared
via
solvent-drop
(water)
grinding
(SDG)
on
multigram
scale
with
97%
yield
characterized
using
FTIR,
1H
NMR,
SCXRD.
The
pyridyl
carboxylate
moiety
present
in
make
suitable
for
use
as
linker
ligand
indeed
found
coordinate
Cu(II),
Zn(II),
Cd(II)
cations,
enabling
serve
assembly
coordination
polymers.
thereby
formed
1D
(spiro
chain)
2D
(square
lattice,
sql,
topology)
polymers
solvent-induced
(layering
slurry)
methods.
resulting
were
though
X-ray
diffraction
(SCXRD,
PXRD)
TGA,
further
demonstrating
utility
green
methods
preparation
some
classes
new
ligands
turn
be
used
Bulletin of the Chemical Society of Japan,
Год журнала:
2025,
Номер
98(3)
Опубликована: Март 1, 2025
Abstract
Alectinib,
which
is
marketed
under
the
name
Alecensa,
an
orally
administered
and
highly
potent
anaplastic
lymphoma
kinase
(ALK)
inhibitor
used
for
treatment
of
ALK-positive
non-small-cell
lung
cancer.
The
distinctive
structural
feature
alectinib
its
indole-fused
tetracyclic
scaffold,
efficient
synthesis
method
crucial
in
establishing
manufacturing
process.
While
methodology
developed
first-in-human
study
has
proved
to
be
practical
preparation
indole-core
on
a
multi-kilogram
scale,
continuous
improvements
process
indole
intermediate
have
been
made
reducing
environmental
impacts
future
campaigns
as
well
sustainable
production
alectinib.
As
result,
newly
established
successfully
eliminates
use
harmful
solvents
restricted
EU
REACH
regulation,
need
rare
earth
element.
Journal of the American Chemical Society,
Год журнала:
2025,
Номер
unknown
Опубликована: Март 12, 2025
Electrochemical
methodologies
offer
a
transformative
approach
to
sustainable
chemical
synthesis
by
enabling
precise,
energy-efficient
transformations.
Here,
we
report
the
selective
electrochemical
N-formylation
of
methylamine
using
methanol
as
both
reagent
and
solvent,
facilitated
simple
glassy
carbon
electrode.
Under
optimized
conditions,
achieve
faradaic
efficiency
(FE)
34%
for
methylformamide
in
neutral
NaClO4
electrolyte.
Mechanistic
insights
from
situ
Fourier-transform
infrared
spectroscopy
(FTIR)
complementary
synthetic
experiments
reveal
two
distinct
reaction
pathways:
direct
oxidation
hemiaminal
intermediate
novel
route
involving
formation
methylisocyanide,
which
subsequently
hydrates
yield
methylformamide.
The
presence
methylisocyanide
was
confirmed
through
mass
spectrometry
analysis
following
successful
Ugi
multicomponent
reaction,
demonstrating
ability
safely
utilize
reactive
intermediates
within
an
framework.
This
work
underscores
potential
electrosynthesis
unlock
metal-free,
pathways
produce
value-added
nitrogen-containing
compounds,
paving
way
greener
approaches
manufacturing
catalysis.
While
the
allyloxycarbonyl
(Alloc)
protecting
group
has
played
a
key
role
in
solid-phase
peptide
synthesis
(SPPS),
providing
access
to
wide
range
of
peptides,
its
removal
suffered
from
relying
on
air-sensitive
Pd(0)
complexes
hazardous
solvents.
We
report
metal-free,
on-resin
Alloc
using
readily
available
iodine/water
environmentally
sensible
PolarClean
(PC)/ethyl
acetate
(EtOAc)
carried
out
one-pot
manner
with
racemization-free
couplings
employing
both
9-fluorenylmethoxycarbonyl
(Fmoc)
and
amino
acids
(AAs).
SPPS
been
demonstrated
by
performing
consecutive
removals–peptide
couplings,
whereas
compatibility
long
peptides
proven
carrying
an
removal–coupling
39
AA
resin.
Upscaling
10
g
was
combined
TFA-free
resin
cleavage,
opening
up
opportunities
for
Alloc-AAs
as
synthons
sustainable
manufacturing.
Journal of Peptide Science,
Год журнала:
2025,
Номер
31(6)
Опубликована: Май 1, 2025
A
revolution
in
peptide
production
arrived
from
the
innovation
of
carboxylate
to
amine
C-
N-direction
solid-phase
synthesis.
This
cornerstone
modern
science
has
enabled
multiple
academic
and
industrial
applications;
however,
process
N-solid
phase
synthesis
(C-N-SPPS)
extreme
mass
intensity
poor
atom
economy.
Notably,
C-N-SPPS
relies
upon
use
atom-intensive
protecting
groups,
such
as
fluorenylmethyloxycarbonyl
(Fmoc)
protection
wasteful
excess
protected
amino
acids
coupling
agents.
On
other
hand,
N-
C-direction
offers
potential
minimize
may
arguably
enable
more
efficient
means
for
manufacturing
peptides.
For
example,
amide
bond
formation
been
accomplished
using
methods
employing
thioesters,
vinyl
esters,
transamidation
achieve
with
minimal
epimerization.
review
aims
provide
an
overview
C-peptide
indicating
advantages
taking
this
avenue
sustainable
production.
