Generation and Use of Bicyclo[1.1.0]butyllithium under Continuous Flow Conditions
Organic Letters,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 20, 2025
The
bicyclo[1.1.0]butyl
scaffold
has
emerged
as
a
valuable
bioisostere
in
drug
discovery
programs.
Here,
we
present
streamlined
approach
for
the
generation
of
bicyclo[1.1.0]butyllithium
and
its
functionalization
with
various
classes
electrophiles
one-flow
process,
eliminating
need
intermediate
isolation.
In
comparison
to
traditional
batch
processes,
flow
method
allows
use
single
organolithium
reagent
instead
two
operates
at
significantly
higher
temperatures
(0
°C
versus
−78
°C),
enhancing
both
practicality
scalability.
Language: Английский
Generation and Use of Cyclopropenyllithium under Continuous Flow Conditions
Organic Letters,
Journal Year:
2025,
Volume and Issue:
unknown
Published: May 21, 2025
The
cyclopropene
scaffold
has
emerged
as
a
valuable
platform
in
modern
synthesis.
Here,
we
present
streamlined
flow-based
approach
for
the
generation
of
cyclopropenyllithium
and
its
functionalization
with
various
electrophiles
single,
continuous
flow
process.
This
method
eliminates
need
laborious
temperature
changes
cryogenic
conditions,
significantly
reduces
process
time
from
starting
material
to
products.
Compared
traditional
batch
processes,
our
enables
use
single
organolithium
reagent
operates
efficiently
at
0
°C,
avoiding
cool-warm-cool
cycles
typical
methods.
not
only
simplifies
workflow
but
also
enhances
practicality,
scalability,
extends
accessible
chemical
space.
Language: Английский
Scalable Synthesis of 1,5-Diazabicyclo[3.1.0]hexanes Using N-Chlorosuccinimide as Chlorinating Agent
Organic Letters,
Journal Year:
2025,
Volume and Issue:
unknown
Published: May 27, 2025
An
optimized
synthetic
approach
toward
the
assembly
of
1,5-diazabicyclo[3.1.0]hexanes
(bicyclic
diaziridines)
was
developed.
This
protocol
involves
utilization
N-chlorosuccinimide
as
a
convenient
and
easy-to-handle
chlorinating
agent,
which
in
combination
with
carbonyl
compounds
1,3-diaminopropane
enables
preparation
wide
set
target
diaziridines.
High
yields,
structural
diversity
scalability
demonstrate
broad
applicability
this
procedure
for
further
investigations.
Language: Английский