This
chapter
focus
on
the
developments
concerning
strategies
used
in
synthesis
of
1,4-diazepane
derivatives
reflecting
selected
relevant
examples
described
literature
between
2005
and
end
2020.
Chiral
1,4-diazepanes
can
be
synthesized
by
asymmetric
reductive
amination,
one
most
important
reactions
to
prepare
chiral
amines.
The
Mitsunobu
reaction
consists
conversion
activated
primary
or
secondary
alcohols,
through
a
dehydrative
coupling,
into
variety
functional
groups
namely
amines,
esters,
phenyl
ethers,
thioethers.
Huisgen
1,3-dipolar
cycloaddition
has
been
preferred
obtain
N-heterocycles
containing
moiety
taking
advantage
N-propargylamines
versatility
as
building
blocks.
One-pot
employing
three
more
different
starting
materials
leading
products
that
incorporate
atoms
from
reagents
are
called
multicomponent
reactions.
Transamination
often
key
intermediates
for
development
pharmaceuticals.
Chemical Reviews,
Journal Year:
2017,
Volume and Issue:
117(24), P. 14091 - 14200
Published: Nov. 22, 2017
Propargylamines
are
a
versatile
class
of
compounds
which
find
broad
application
in
many
fields
chemistry.
This
review
aims
to
describe
the
different
strategies
developed
so
far
for
synthesis
propargylamines
and
their
derivatives
as
well
highlight
reactivity
use
building
blocks
chemically
relevant
organic
compounds.
In
first
part
review,
synthetic
approaches
synthesize
propargylamines,
such
A3
couplings
C–H
functionalization
alkynes,
have
been
described
organized
on
basis
catalysts
employed
syntheses.
Both
racemic
enantioselective
reported.
second
part,
an
overview
transformations
into
heterocyclic
pyrroles,
pyridines,
thiazoles,
oxazoles,
other
derivatives,
is
presented.
ACS Catalysis,
Journal Year:
2023,
Volume and Issue:
13(14), P. 9442 - 9475
Published: July 3, 2023
Spirocyclic
indole
derivatives
are
fascinating
tridimensional
molecular
scaffolds
from
both
a
synthetic
and
biological
point
of
view.
Among
the
many
strategies
developed
to
access
these
structures,
transition
metal
catalysis
has
recently
led
impressive
advances,
especially
relying
on
unique
reactivity
dearomatized
spirocyclic
intermediates.
These
species
can
indeed
evolve
toward
or
nonspirocyclic
products
through
rearomatization-driven
processes,
which
at
same
time
highly
challenging
control
but
also
source
large
structural
diversity.
This
review
highlights
most
prominent
methods
past
decade
that
involve
spirocyclization
tethered
functional
group
may
be
activated
by
metal,
leading
rearomatized
products.
The
discussion
is
particularly
focused
spiroindoleninium
intermediate
complex
mechanistic
features
regarding
its
evolution,
dependent
catalytic
systems.
European Journal of Organic Chemistry,
Journal Year:
2018,
Volume and Issue:
2018(17), P. 1925 - 1945
Published: April 16, 2018
This
review
summarizes
the
progress
achieved
in
last
fifteen
years
by
application
of
homogeneous
gold
catalysis
field
indole
functionalization.
Several
electrophilic
species
obtained
through
gold‐catalyzed
π‐activation
have
fact
been
found
to
react
with
nucleophilic
positions
indole,
thus
allowing
its
efficient
manipulation.
In
order
furnish
a
complete
and
clear
overview
on
role
catalyst,
is
organized
from
perspective
gold‐activated
substrate
that
reacting
indole.
addition,
view
ability
catalyze
tandem
cascade
reactions,
separate
section
describes
tandem/cascade
protocols
useful
for
synthesis
complex
polycyclic
derivatives.
Finally,
has
also
employed
indole‐based
natural
products.
For
this
reason,
dedicated
collects
all
work
which
key
step
obtain
these
indoles
represented
reaction.
RSC Advances,
Journal Year:
2016,
Volume and Issue:
6(102), P. 99781 - 99793
Published: Jan. 1, 2016
N-Propargylamines
are
one
of
the
most
useful
and
versatile
building
blocks
in
organic
synthesis
that
successfully
transformed
into
many
significant
N-heterocycles.
Green Chemistry,
Journal Year:
2017,
Volume and Issue:
19(16), P. 3851 - 3855
Published: Jan. 1, 2017
A
method
for
the
catalyst-free
synthesis
of
pyrroloquinolinediones
and
quinolinedicarboxylates
is
developed
through
a
one-pot
involving
denitrogenation
azide,
benzisoxazole
formation,
aza-Diels–Alder
cycloaddition,
dehydrative
aromatization.
Only
stoichiometric
amounts
N2
H2O
are
produced
as
by-products.
comprehensive
green
chemistry
metrics
analysis
indicated
that
this
much
more
efficient
greener
than
two
reported
methods
pyrroloquinolinediones.
Chemistry - A European Journal,
Journal Year:
2020,
Volume and Issue:
27(4), P. 1165 - 1218
Published: June 30, 2020
Heteroarene-tethered
functionalized
alkynes
are
multipotent
synthons
in
organic
chemistry.
This
detailed
Review
described
herein
offers
a
thorough
discussion
of
the
metamorphosis
heteroarene-tethered
alkynes,
an
area
which
has
earned
much
attention
over
past
decade
straightforward
synthesis
architecturally
complex
heterocyclic
scaffolds
atom
and
step
economic
manner.
Depending
upon
variety
this
is
divided
into
multiple
sections.
Amongst
vast
array
synthetic
transformations
covered,
dearomatizing
spirocyclizations
cascade
spirocyclization/rearrangement
great
interest.
Synthetic
involving
with
scope,
challenges,
limitations,
mechanism,
their
application
total
natural
products
future
perceptions
surveyed.
Synthetic Communications,
Journal Year:
2021,
Volume and Issue:
51(24), P. 3694 - 3716
Published: Nov. 12, 2021
Research
on
the
synthesis
of
heterocyclic
compounds
is
always
a
hot
research
topic
among
synthetic
chemists,
because
heterocycles
are
very
important
scaffolds
in
structure
numerous
drugs,
natural
products
and
biologically
active
molecules.
Propargylamines
versatile
class
amine
which
find
many
applications
different
fields
chemistry
such
as
chemistry.
In
recent
times,
utilization
propargylamines
reagent
for
have
received
profound
attention
organic
synthesis.
This
review
will
provide
comprehensive
knowledge
efficient
reagents
compounds.
ChemistrySelect,
Journal Year:
2023,
Volume and Issue:
8(17)
Published: May 2, 2023
Abstract
A
series
of
derivative
benzimidazol‐2‐thione
compounds
(
2
a–2
l
)
had
been
synthesized,
screened
for
their
antimicrobial
activities
by
dish
diffusion
and
dilution
assays,
anti‐tumor
against
breast,
rhabdomyosarcoma,
liver
human
cancer
cell
lines
via
MTT
assay,
followed
carrying
out
in
silico
docking
model.
Entries
i–2
j,
,
g
are
novel
compounds,
among
them,
compound
2i
manifested
the
highest
antibacterial
activity
both
Methicillin‐resistant
Staphylococcus
aureus
Streptococcus
faecalis
;
meanwhile,
entries
j
showed
significant
antifungal
toward
Trichophyton
mentagrophytes
rubrum
Microsporum
gypseum
.
Through
vitro
approach,
entry
i
is
best
rhabdomyosarcoma
line.
Additionally,
reasonably
explained
drug
delivery
ligand
bacterium
moreover,
excellent
activity,
enzyme
inhibition
mechanism
2VF5.
In
was
proved
to
inhibit
sarcoma
Advanced Synthesis & Catalysis,
Journal Year:
2018,
Volume and Issue:
360(21), P. 4037 - 4042
Published: July 19, 2018
Abstract
An
efficient
copper‐catalyzed
cyclization
of
o
‐azidobenzaldehyde
and
nitro‐olefins
was
developed.
This
reaction
proceeds
under
solvent‐free
conditions
displays
broad
functional
group
compatibility
affords
3‐nitroquinolines
in
good
to
excellent
yields.
The
synthetic
utility
this
strategy
is
illustrated
by
the
concise
construction
quindolines
only
three
steps,
which
renders
more
practical.
magnified
image
