Advanced Synthesis & Catalysis,
Journal Year:
2023,
Volume and Issue:
365(24), P. 4359 - 4391
Published: Nov. 7, 2023
Abstract
Amide
bond
construction
has
garnered
significant
interest
in
recent
decades
due
to
amides
being
one
of
the
most
prevalent
functional
groups
among
bioactive
molecules.
Out
thirty‐seven
new
drugs
approved
by
FDA
2022,
eleven
are
small
molecules
containing
at
least
amide
bond.
Additionally,
there
nineteen
large
as
drugs,
some
which
have
peptide
structures,
and
therefore,
also
bear
bonds.
In
years,
multiple
teams
embraced
challenge
developing
more
efficient
methods
for
formation.
This
dedication
led
numerous
publications
appearing
monthly
prestigious
journals,
showcasing
advancements
this
field.
The
primary
goal
review
is
present
viable
strategies
constructing
It
crucial
differentiate
between
formation
synthesis;
hence,
focus
on
describing
specific
forming
C(O)−N
particular,
concentrates
developed
within
last
six
years.
There
a
particular
emphasis
approaches
that
consider
thought
process
when
selecting
starting
materials
groups.
approach
ensures
coverage
all
common
chemical
transformations
yield
The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
89(7), P. 4261 - 4282
Published: March 20, 2024
Small
molecule
therapeutics
represent
the
majority
of
FDA-approved
drugs.
Yet,
many
attractive
targets
are
poorly
tractable
by
small
molecules,
generating
a
need
for
new
therapeutic
modalities.
Due
to
their
biocompatibility
profile
and
structural
versatility,
peptide-based
possible
solution.
Additionally,
in
past
two
decades,
advances
peptide
design,
delivery,
formulation,
devices
have
occurred,
making
peptides
an
modality.
However,
manufacturing
is
often
limited
solid-phase
synthesis
(SPPS),
liquid
phase
(LPPS),
lesser
extent
hybrid
SPPS/LPPS,
with
SPPS
emerging
as
predominant
platform
technology
synthesis.
involves
use
excess
solvents
reagents
which
negatively
impact
environment,
thus
highlighting
newer
technologies
reduce
environmental
footprint.
Herein,
fourteen
American
Chemical
Society
Green
Chemistry
Institute
Pharmaceutical
Roundtable
(ACS
GCIPR)
member
companies
portfolio
compiled
Process
Mass
Intensity
(PMI)
metrics
help
inform
sustainability
efforts
This
includes
PMI
assessment
on
40
synthetic
processes
at
various
development
stages
pharma,
classified
according
phase.
most
comprehensive
date.
The
process
was
divided
into
(synthesis,
purification,
isolation)
determine
respective
PMI.
On
average,
(SPPS)
(PMI
≈
13,000)
does
not
compare
favorably
other
modalities
such
molecules
median
168–308)
biopharmaceuticals
8300).
Thus,
high
warrants
more
environmentally
friendly
manufacturing.
Chemical Science,
Journal Year:
2023,
Volume and Issue:
14(13), P. 3462 - 3469
Published: Jan. 1, 2023
Technology
for
generating
especially
important
amide
and
peptide
bonds
from
carboxylic
acids
amines
that
avoids
traditional
coupling
reagents
is
described.
The
1-pot
processes
developed
rely
on
thioester
formation,
neat,
using
a
simple
dithiocarbamate,
are
safe
green,
Nature-inspired
thioesters
then
converted
to
the
targeted
functionality.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(12), P. 4809 - 4809
Published: June 16, 2023
Many
years
ago,
twelve
principles
were
defined
for
carrying
out
chemical
reactions
and
processes
from
a
green
chemistry
perspective.
It
is
everyone’s
endeavor
to
take
these
points
into
account
as
far
possible
when
developing
new
or
improving
existing
ones.
Especially
in
the
field
of
organic
synthesis,
area
research
has
thus
been
established:
micellar
catalysis.
This
review
article
addresses
question
whether
catalysis
by
applying
reaction
media.
The
shows
that
many
can
be
transferred
an
solvent
medium,
but
surfactant
also
crucial
role
solubilizer.
Thus,
carried
much
more
environmentally
friendly
manner
with
less
risk.
Moreover,
surfactants
are
being
reformulated
their
design,
degradation
add
extra
advantages
match
all
chemistry.
Organic Process Research & Development,
Journal Year:
2023,
Volume and Issue:
27(1), P. 120 - 128
Published: Jan. 9, 2023
Herein,
the
amide
coupling
of
six
primary
amines
with
sodium
salt
diazabicyclooctane
acid
in
an
aqueous
medium
without
additional
base/surfactant
or
organic
solvent
is
described.
The
product
was
efficiently
isolated
from
reaction
through
simple
filtration
and
recrystallized
using
hot
water
treatment
as
a
swift
cost-effective
process.
methodology
implemented
on
kilogram
scale
to
produce
penultimate
intermediates
for
synthesizing
β-lactamase
inhibitors
such
zidebactam,
relebactam,
nacubactam.
comparison
green
metrics
several
previously
reported
methods
discussed.
developed
procedure
avoids
hazardous
solvents
provides
isolation
method
at
operational
level
high
purity
efficiency.
