Organic Process Research & Development,
Journal Year:
2024,
Volume and Issue:
28(11), P. 4034 - 4038
Published: Oct. 21, 2024
A
simple
and
widely
applicable
technique
to
avoid
precipitation-induced
clogging
in
continuous-flow
processes
involving
gas
liquid
reagents
(such
as
hydrogenations)
has
been
developed.
Management
of
solid
compounds
poses
one
the
largest
scale-up
risks
flow
manufacturing
pharmaceuticals
fine
chemicals.
As
noted
this
study,
with
limited
solubility
low-boiling
solvents
can
be
susceptible
precipitation
when
mixed
a
stream
standard
tee-mixer.
The
prescribed
technique,
whereby
is
prewetted
solvent
prior
contacting
feed
solution,
successfully
applied
both
lab
platforms
enhance
stable
(clog-free)
operating
run
time
synthesis
an
active
pharmaceutical
ingredient
(API)
intermediate
from
minutes
days.
Bulletin of the Chemical Society of Japan,
Journal Year:
2023,
Volume and Issue:
96(8), P. 752 - 758
Published: June 26, 2023
Abstract
Gas–liquid
phase
reactions
have
proven
invaluable
for
molecular
transformations
in
laboratory
and
industrial
applications.
However,
despite
their
advantages,
the
high
pressure
vigorous
agitation
that
are
required
to
increase
dissolved
gas
concentration
hinder
possible
Application
of
fine
bubbles
(FBs),
which
a
diameter
smaller
than
100
µm,
enables
gas-involved
under
mild
conditions.
In
this
study,
we
quantified
evaluated
reactivities
FBs
gases
various
FB
The
photooxidation
sulfide
using
O2-FB-generated
sulfoxide
depends
on
O2;
meanwhile,
H2-FB-mediated
hydrogenation
alkenes
with
Pd
catalyst
produced
higher
yields
expected
from
H2.
gas–liquid–solid
reaction,
metal
may
form
tunnel
between
neighboring
local
concentration,
providing
yields.
applicability
effect
was
via
deactivated
presence
H2-FBs,
led
recovery
poisoning.
research
findings
demonstrated
surface
play
crucial
role
enhancing
reactivity
involves
solid
phases.
addition,
executed
FB-mediated
poisoned
demonstrate
ability
suppress
Organic Process Research & Development,
Journal Year:
2024,
Volume and Issue:
28(8), P. 3273 - 3283
Published: July 31, 2024
Azvudine
was
approved
for
the
treatment
of
adult
HIV-1
infection
in
China
2021,
and
it
conditional
marketing
SARS-CoV-2
2022.
In
this
work,
we
describe
a
fully
continuous
flow
synthesis
2′-deoxy-2′-fluoroarabinoside,
key
intermediate
azvudine.
The
process
accomplished
via
six
chemical
transformations,
including
chlorination,
hydrolysis,
fluorination,
bromination,
condensation,
deprotection
sequential
devices.
Under
optimized
conditions,
total
yield
32.3%
with
residence
time
156
min.
Compared
batch
doubled,
reaction
shortened
16
times,
E
factor
reduced
1.63
times.
Organic Process Research & Development,
Journal Year:
2024,
Volume and Issue:
28(11), P. 4034 - 4038
Published: Oct. 21, 2024
A
simple
and
widely
applicable
technique
to
avoid
precipitation-induced
clogging
in
continuous-flow
processes
involving
gas
liquid
reagents
(such
as
hydrogenations)
has
been
developed.
Management
of
solid
compounds
poses
one
the
largest
scale-up
risks
flow
manufacturing
pharmaceuticals
fine
chemicals.
As
noted
this
study,
with
limited
solubility
low-boiling
solvents
can
be
susceptible
precipitation
when
mixed
a
stream
standard
tee-mixer.
The
prescribed
technique,
whereby
is
prewetted
solvent
prior
contacting
feed
solution,
successfully
applied
both
lab
platforms
enhance
stable
(clog-free)
operating
run
time
synthesis
an
active
pharmaceutical
ingredient
(API)
intermediate
from
minutes
days.
