The Innovation,
Год журнала:
2024,
Номер
5(2), С. 100586 - 100586
Опубликована: Фев. 3, 2024
The
chemical
recycling
of
polyolefin
presents
a
considerable
challenge,
especially
as
upcycling
methods
struggle
with
the
reality
that
plastic
wastes
typically
consist
mixtures
polyethylene
(PE),
polystyrene
(PS),
and
polypropylene
(PP).
We
report
catalytic
aerobic
oxidative
approach
for
polyolefins
corresponding
carboxylic
acids
product.
This
method
encompasses
three
key
innovations.
First,
it
operates
under
atmospheric
pressure
mild
conditions,
using
O
Journal of the American Chemical Society,
Год журнала:
2024,
Номер
146(4), С. 2845 - 2854
Опубликована: Янв. 18, 2024
In
this
report,
we
developed
a
unified
and
standardized
one-pot
sequence
that
converts
pyridine
derivatives
into
1,2-diazepines
by
inserting
nitrogen
atom.
This
skeletal
transformation
capitalizes
on
the
in
situ
generation
of
1-aminopyridinium
ylides,
which
rearrange
under
UV
light
irradiation.
A
thorough
evaluation
key
parameters
(wavelength,
reaction
conditions,
activating
agent)
allowed
us
to
elaborate
simple,
mild,
user-friendly
protocol.
The
model
was
extrapolated
more
than
40
examples,
including
drug
derivatives,
affording
unique
7-membered
structures.
Mechanistic
evidence
supports
transient
presence
diazanorcaradiene
species.
Finally,
pertinent
transformations
products,
ring
contraction
reactions
form
pyrazoles,
were
conducted
paved
way
broad
application
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
67(14), С. 11459 - 11466
Опубликована: Июнь 21, 2024
ADVERTISEMENT
RETURN
TO
ARTICLES
ASAPPREVEditorialNEXTRational
Molecular
Editing:
A
New
Paradigm
in
Drug
DiscoveryChunhua
MaChunhua
MaState
Key
Laboratory
of
Antiviral
Drugs,
Pingyuan
Laboratory,
NMPA
for
Research
and
Evaluation
Innovative
Drug,
School
Chemistry
Chemical
Engineering,
Henan
Normal
University,
Xinxiang,
453007,
ChinaMore
by
Chunhua
Mahttps://orcid.org/0000-0001-7613-6471,
Craig
W.
Lindsley*Craig
LindsleyVanderbilt
University
Medical
Center,
Franklin,
Tennessee
37027,
United
States*E-mail:
[email
protected]More
Lindsleyhttps://orcid.org/0000-0003-0168-1445,
Junbiao
Chang*Junbiao
ChangCollege
Chemistry,
State
Zhengzhou
450001,
China*E-mail:
Chang,
Bin
Yu*Bin
YuCollege
Yuhttps://orcid.org/0000-0002-7207-643XCite
this:
J.
Med.
Chem.
2024,
XXXX,
XXX,
XXX-XXXPublication
Date
(Web):June
21,
2024Publication
History
Received13
June
2024Published
online21
2024https://pubs.acs.org/doi/10.1021/acs.jmedchem.4c01347https://doi.org/10.1021/acs.jmedchem.4c01347editorialACS
PublicationsPublished
2024
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Get
e-AlertscloseSUBJECTS:Drug
discovery,Macrocyclization,Molecules,Pharmaceuticals,Scaffolds
e-Alerts
Journal of the American Chemical Society,
Год журнала:
2024,
Номер
146(7), С. 4301 - 4308
Опубликована: Фев. 9, 2024
The
development
of
divergent
methods
to
expedite
structure–activity
relationship
studies
is
crucial
streamline
discovery
processes.
We
developed
a
rare
example
regiodivergent
ring
expansion
access
two
regioisomers
from
common
starting
material.
To
enable
this
regiodivergence,
we
identified
distinct
reaction
conditions
for
transforming
oxindoles
into
quinolinone
isomers.
presented
proved
be
compatible
with
variety
functional
groups,
which
enabled
the
late-stage
diversification
bioactive
as
well
facilitated
synthesis
drugs
and
their
derivatives.
Science,
Год журнала:
2025,
Номер
387(6729), С. 102 - 107
Опубликована: Янв. 2, 2025
Given
the
prevalence
of
nitrogen-containing
heterocycles
in
commercial
drugs,
selectively
incorporating
a
single
nitrogen
atom
is
promising
scaffold
hopping
approach
to
enhance
chemical
diversity
drug
discovery
libraries.
We
harness
distinct
reactivity
sulfenylnitrenes,
which
insert
transform
readily
available
pyrroles,
indoles,
and
imidazoles
into
synthetically
challenging
pyrimidines,
quinazolines,
triazines,
respectively.
Our
additive-free
method
for
skeletal
editing
employs
easily
accessible,
benchtop-stable
sulfenylnitrene
precursors
over
broad
temperature
range
(−30
150°C).
This
compatible
with
diverse
functional
groups,
including
oxidation-sensitive
functionalities
such
as
phenols
thioethers,
has
been
applied
various
natural
products,
amino
acids,
pharmaceuticals.
Furthermore,
we
have
conducted
mechanistic
studies
explored
regioselectivity
outcomes
through
density
theory
calculations.
Chemistry - A European Journal,
Год журнала:
2023,
Номер
29(24)
Опубликована: Фев. 2, 2023
Skeletal
editing
via
single-atom
insertion
reactions
involving
nitrogen
heterocycles
have
been
reported
by
two
innovative
and
complementary
methods
for
the
conversion
of
pyrroles
indoles
to
pyridines,
quinolines
quinazolines.
The
use
electrophilic
carbonyl
cation
equivalents
in
situ
generated
nitrenes
enables
molecular
transform
forming
foundation
best-selling
pharmaceuticals.
Considering
importance
medicinal
chemistry,
biology
natural
products,
these
offer
approach
complex
structures
heterocycle
diversification
peripheral
editing.
Journal of the American Chemical Society,
Год журнала:
2023,
Номер
145(32), С. 17570 - 17576
Опубликована: Авг. 3, 2023
In
this
study,
we
describe
the
direct
insertion
of
an
intramolecular
nitrogen
atom
into
aromatic
C–C
bond.
transformation,
carbamoyl
azides
are
activated
by
a
Rh
catalyst
and
subsequently
directly
inserted
bond
arene
ring
to
access
fused
azepine
products.
This
transformation
is
challenging,
owing
existence
competitive
C–H
amination
pathway.
The
use
paddlewheel
dirhodium
complex
Rh2(esp)2
effectively
inhibited
undesired
insertion.
Density
functional
theory
calculations
were
performed
reveal
reaction
mechanism
origin
chemoselectivity
Rh-catalyzed
reactions.
novel
products
highly
robust
allow
for
downstream
diversification.
Acta Pharmaceutica Sinica B,
Год журнала:
2023,
Номер
14(3), С. 1030 - 1076
Опубликована: Ноя. 18, 2023
Synthetic
chemistry
plays
an
indispensable
role
in
drug
discovery,
contributing
to
hit
compounds
identification,
lead
optimization,
candidate
drugs
preparation,
and
so
on.
As
Nobel
Prize
laureate
James
Black
emphasized,
"the
most
fruitful
basis
for
the
discovery
of
a
new
is
start
with
old
drug"