Bioresources and Bioprocessing,
Journal Year:
2022,
Volume and Issue:
9(1)
Published: Jan. 24, 2022
Terpenoids
form
the
most
diversified
class
of
natural
products,
which
have
gained
application
in
pharmaceutical,
food,
transportation,
and
fine
bulk
chemical
industries.
Extraction
from
naturally
occurring
sources
does
not
meet
industrial
demands,
whereas
synthesis
is
often
associated
with
poor
enantio-selectivity,
harsh
working
conditions,
environmental
pollutions.
Microbial
cell
factories
come
as
a
suitable
replacement.
However,
designing
efficient
microbial
platforms
for
isoprenoid
challenging
task.
This
has
to
do
cytotoxic
effects
pathway
intermediates
some
end
instability
expressed
pathways,
well
high
enzyme
promiscuity.
Also,
low
enzymatic
activity
terpene
synthases
prenyltransferases,
lack
an
throughput
system
screen
improved
high-performing
strains
are
bottlenecks
strain
development.
Metabolic
engineering
synthetic
biology
seek
overcome
these
issues
through
provision
effective
tools.
review
sought
provide
in-depth
description
novel
strategies
improving
factory
performance.
We
focused
on
transcriptional
translational
efficiencies
static
dynamic
regulatory
elements,
high-throughput
screening
strategies,
cellular
function
enhancement
chromosomal
integration,
metabolite
tolerance,
modularization
pathways.
ACS Catalysis,
Journal Year:
2021,
Volume and Issue:
11(5), P. 2684 - 2690
Published: Feb. 12, 2021
The
construction
of
N-heterocyclic
eight-membered
rings
with
good
regio-,
stereo-,
and
enantioselective
control
remains
a
formidable
challenge
in
asymmetric
catalysis.
Herein,
we
report
palladium-catalyzed
[4
+
4]
cycloaddition
anthranils
γ-methylidene-δ-valerolactones
the
presence
Et3B,
delivering
highly
functionalized
tetrahydrobenzo[b]azocine
derivatives
high
efficiency
diastereoselectivities
enantioselectivities
(up
to
92%
yield,
20:1
dr,
99%
ee).
Moreover,
complex
substrates
derived
from
natural
products
(bearing
different
functionalities)
could
be
well-tolerated
catalytic
cycloaddition.
mild
reaction
conditions,
conjunction
broad
substrate
scope
(44
examples),
level
stereoselectivity,
provide
great
potential
build
azocine
compounds
simple
building
blocks.
Journal of the American Chemical Society,
Journal Year:
2021,
Volume and Issue:
143(42), P. 17366 - 17373
Published: Oct. 12, 2021
We
report
here
a
reaction
that
selectively
deaminates
primary
amines
and
anilines
under
mild
conditions
with
remarkable
functional
group
tolerance
including
range
of
pharmaceutical
compounds,
amino
acids,
sugars,
natural
products.
An
anomeric
amide
reagent
is
uniquely
capable
facilitating
the
through
intermediacy
an
unprecedented
monosubstituted
isodiazene
intermediate.
In
addition
to
dramatically
simplifying
deamination
compared
existing
protocols,
our
approach
enables
strategic
applications
iminium
amine-directed
chemistries
as
traceless
methods.
Mechanistic
computational
studies
support
intermedicacy
which
exhibits
unexpected
divergence
from
previously
studied
secondary
isodiazenes,
leading
cage-escaping,
free
radical
species
engage
in
chain,
hydrogen-atom
transfer
process
involving
aliphatic
diazenyl
intermediates.
Organic Chemistry Frontiers,
Journal Year:
2022,
Volume and Issue:
10(1), P. 216 - 236
Published: Nov. 8, 2022
The
late
stage
functionalization
(LSF)
is
a
distinctive
approach
for
accelerating
the
discovery
of
structure–activity
relationships
(SARs)
and
optimising
ADME
(absorption,
distribution,
metabolism,
excretion)
profiles.
Molecules,
Journal Year:
2022,
Volume and Issue:
27(3), P. 1003 - 1003
Published: Feb. 2, 2022
Late-stage
modification
of
drug
molecules
is
a
fast
method
to
introduce
diversity
into
the
already
biologically
active
scaffold.
A
notable
number
analogs
mefloquine,
chloroquine,
and
hydroxychloroquine
have
been
synthesized,
starting
from
readily
available
pharmaceutical
ingredient
(API).
In
current
review,
all
modifications
sites
reactivity
types
are
summarized
provide
insight
chemistry
these
molecules.
The
approaches
include
introduction
simple
groups
functionalities.
Coupling
other
drugs,
polymers,
or
carriers
afforded
hybrid
compounds
conjugates
with
either
easily
hydrolyzable
more
chemically
inert
bonds.
utility
some
was
tested
in
antiprotozoal,
antibacterial,
antiproliferative
assays,
as
well
enantiodifferentiation
experiments.
Bioresources and Bioprocessing,
Journal Year:
2022,
Volume and Issue:
9(1)
Published: Jan. 24, 2022
Terpenoids
form
the
most
diversified
class
of
natural
products,
which
have
gained
application
in
pharmaceutical,
food,
transportation,
and
fine
bulk
chemical
industries.
Extraction
from
naturally
occurring
sources
does
not
meet
industrial
demands,
whereas
synthesis
is
often
associated
with
poor
enantio-selectivity,
harsh
working
conditions,
environmental
pollutions.
Microbial
cell
factories
come
as
a
suitable
replacement.
However,
designing
efficient
microbial
platforms
for
isoprenoid
challenging
task.
This
has
to
do
cytotoxic
effects
pathway
intermediates
some
end
instability
expressed
pathways,
well
high
enzyme
promiscuity.
Also,
low
enzymatic
activity
terpene
synthases
prenyltransferases,
lack
an
throughput
system
screen
improved
high-performing
strains
are
bottlenecks
strain
development.
Metabolic
engineering
synthetic
biology
seek
overcome
these
issues
through
provision
effective
tools.
review
sought
provide
in-depth
description
novel
strategies
improving
factory
performance.
We
focused
on
transcriptional
translational
efficiencies
static
dynamic
regulatory
elements,
high-throughput
screening
strategies,
cellular
function
enhancement
chromosomal
integration,
metabolite
tolerance,
modularization
pathways.
