Chemistry - A European Journal,
Journal Year:
2016,
Volume and Issue:
23(9), P. 2225 - 2230
Published: Dec. 9, 2016
Medium-sized
rings
are
widely
considered
to
be
under-represented
in
biological
screening
libraries
for
lead
identification
medicinal
chemistry.
To
help
address
this,
a
library
of
medium-sized
lactams
has
been
generated
by
using
simple,
scalable
and
versatile
ring-expansion
protocol.
Analysis
the
open-access
computational
tool
LLAMA
suggested
that
these
their
derivatives
have
highly
promising
physicochemical
3D
spatial
properties
thus
much
potential
drug
discovery.
Organic & Biomolecular Chemistry,
Journal Year:
2021,
Volume and Issue:
19(18), P. 3960 - 3982
Published: Jan. 1, 2021
Bridged
polycycles
are
privileged
molecular
skeletons
with
wide
occurrence
in
bioactive
natural
products
and
pharmaceuticals.
Therefore,
they
have
been
the
pursing
target
molecules
of
numerous
chemists.
The
rapid
convenient
generation
sp3-rich
complex
three-dimensional
from
simple
easily
available
aromatics
has
made
dearomatization
a
highly
valuable
synthetic
tool
for
construction
rigid
challenging
bridged
rings.
This
review
summarizes
the-state-of-the-art
advances
strategies
application
ring
formation,
discusses
their
advantages
limitations
in-depth
mechanism,
highlights
value
total
synthesis
products.
We
wish
this
will
provide
an
important
reference
medicinal
chemists
inspire
further
development
intriguing
research
area.
ACS Catalysis,
Journal Year:
2023,
Volume and Issue:
13(2), P. 1164 - 1172
Published: Jan. 4, 2023
The
divergent
construction
of
chiral
medium-sized
rings
is
an
essential
but
challenging
task
in
organic
synthesis.
Herein,
we
report
a
temperature-controlled
catalytic
system
for
the
divergent,
enantioselective
synthesis
different
types
starting
from
same
substrate
set.
Enabled
by
planar
bisphosphine
ligand,
palladium-catalyzed
(5
+
4)
and
formal
2)
annulations
cyclic
aza-dienes
vinylethylene
carbonates
proceeded
smoothly
to
afford
broad
spectrum
indole-based
heterocycles
excellent
yields
with
outstanding
enantioselectivities.
Those
products
could
be
further
diversified
through
various
functional
group
transformations.
Moreover,
mechanistic
studies,
including
control
experiments
DFT
calculations,
shed
light
on
understanding
observed
regio-
enantioselectivities
n)
cyclization.
Journal of the American Chemical Society,
Journal Year:
2024,
Volume and Issue:
146(8), P. 5702 - 5711
Published: Feb. 19, 2024
Macrocycles
and
medium-sized
rings
are
important
in
many
scientific
fields
technologies
but
hard
to
make
using
current
methods,
especially
on
a
large
scale.
Outlined
herein
is
strategy
by
which
functionalized
macrocycles
can
be
prepared
cyclization/ring
expansion
(CRE)
cascade
reactions,
without
resorting
high
dilution
conditions.
CRE
reactions
designed
operate
exclusively
via
kinetically
favorable
5–7-membered
ring
cyclization
steps;
this
means
that
the
problems
typically
associated
with
classical
end-to-end
macrocyclization
avoided.
A
modular
synthetic
approach
has
been
developed
facilitate
simple
assembly
of
requisite
linear
precursors,
then
converted
into
an
extremely
broad
range
one
nine
protocols.
Angewandte Chemie International Edition,
Journal Year:
2017,
Volume and Issue:
56(14), P. 4002 - 4005
Published: March 7, 2017
Abstract
An
enantioselective
iridium‐catalyzed
allylic
substitution
with
a
set
of
highly
unstabilized
nucleophiles
generated
in
situ
from
2‐methylpyridines
is
described.
Enantioenriched
2‐substituted
pyridines,
which
are
frequently
encountered
natural
products
and
pharmaceuticals,
could
be
easily
constructed
by
this
simple
method
good
yields
excellent
enantioselectivity.
The
synthetic
utility
the
pyridine
demonstrated
through
synthesis
key
intermediate
reported
Na
+
/H
exchanger
inhibitor
total
(−)‐lycopladine
A.
Chemistry - A European Journal,
Journal Year:
2016,
Volume and Issue:
23(9), P. 2225 - 2230
Published: Dec. 9, 2016
Medium-sized
rings
are
widely
considered
to
be
under-represented
in
biological
screening
libraries
for
lead
identification
medicinal
chemistry.
To
help
address
this,
a
library
of
medium-sized
lactams
has
been
generated
by
using
simple,
scalable
and
versatile
ring-expansion
protocol.
Analysis
the
open-access
computational
tool
LLAMA
suggested
that
these
their
derivatives
have
highly
promising
physicochemical
3D
spatial
properties
thus
much
potential
drug
discovery.
