Asian Journal of Organic Chemistry,
Journal Year:
2020,
Volume and Issue:
9(6), P. 898 - 909
Published: May 4, 2020
Abstract
Site‐selective
chemical
modifications
that
target
proteinogenic
amino
acid
residues
complement
the
methods
entailing
genetic
manipulation,
thereby
allowing
straightforward
and
rapid
access
to
engineered
proteins.
The
incorporation
of
trifluoromethyl
group
into
acids
within
a
peptide
sequence
results
in
relevant
peptidomimetics
with
unique
biomedicinal
properties.
As
result,
last
decade
has
witnessed
development
powerful
set
protocols
toward
selective
trifluoromethylation
small‐to‐medium
size
peptides
proteins
late‐stage
fashion.
This
minireview
seeks
highlight
those
particularly
compelling
cases
published
years.
Angewandte Chemie,
Journal Year:
2020,
Volume and Issue:
132(50), P. 22759 - 22765
Published: Sept. 24, 2020
Abstract
The
application
of
piezoelectricity
for
the
generation
trifluoromethyl
(CF
3
)
radicals
is
reported
together
with
development
a
method
mechanochemical
C−H
trifluoromethylation
aromatic
compounds.
As
compared
to
conventional
solution‐based
approaches,
this
mechanoredox
enables
cleaner
and
more
sustainable
access
wide
range
trifluoromethylated
N‐heterocycles
peptides,
which
are
important
structural
motifs
in
modern
drug
discovery.
This
study
thus
represents
an
milestone
future
applications
systems
medicinal
pharmaceutical
science.
Angewandte Chemie International Edition,
Journal Year:
2021,
Volume and Issue:
61(5)
Published: Nov. 30, 2021
Site-selective
peptide
functionalization
provides
a
straightforward
and
cost-effective
access
to
diversify
peptides
for
biological
studies.
Among
many
existing
non-invasive
conjugations
methodologies,
photoredox
catalysis
has
emerged
as
one
of
the
powerful
approaches
site-specific
manipulation
on
native
peptides.
Herein,
we
report
highly
N-termini-specific
method
rapidly
itaconated
their
derivatives
through
combination
transamination
conditions.
This
strategy
exploits
facile
reactivity
peptidyl-dihydropyridine
in
complex
settings,
complementing
bioconjugations
with
excellent
selectivity
under
mild
Distinct
from
conventional
methods,
this
utilizes
reactive
carbamoyl
radical
derived
peptidyl-dihydropyridine.
In
addition,
can
be
further
functionalized
Michael
acceptor
corresponding
peptide-protein
conjugate.
Asian Journal of Organic Chemistry,
Journal Year:
2020,
Volume and Issue:
9(6), P. 898 - 909
Published: May 4, 2020
Abstract
Site‐selective
chemical
modifications
that
target
proteinogenic
amino
acid
residues
complement
the
methods
entailing
genetic
manipulation,
thereby
allowing
straightforward
and
rapid
access
to
engineered
proteins.
The
incorporation
of
trifluoromethyl
group
into
acids
within
a
peptide
sequence
results
in
relevant
peptidomimetics
with
unique
biomedicinal
properties.
As
result,
last
decade
has
witnessed
development
powerful
set
protocols
toward
selective
trifluoromethylation
small‐to‐medium
size
peptides
proteins
late‐stage
fashion.
This
minireview
seeks
highlight
those
particularly
compelling
cases
published
years.
