A novel amino-thiocarbamate-catalyzed bromolactonization of unsaturated carboxylic acids has been developed. The scope of the reaction is evidenced by 22 examples of γ-lactones with up to 99% yield and 93% ee. The protocol was applied in the enantioselective synthesis of the key intermediates of VLA-4 antagonists.
Synthetic
water channels were developed with an aim to replace
aquaporins for possible uses in water purification, while concurrently
retaining aquaporins’ ability to conduct highly selective superfast
water transport. Among the currently available synthetic water channel
systems, none possesses water transport properties that parallel those
of aquaporins. In this report, we present the first synthetic water
channel system with intriguing aquaproin-like features. Employing
a “sticky end”-mediated molecular strategy for constructing
abiotic water channels, we demonstrate that a 20% enlargement in angstrom-scale
pore volume could effect a remarkable enhancement in macroscopic water
transport profile by 15 folds. This gives rise to a powerful synthetic
water channel able to transport water at a speed of ∼3 ×
109 H2O s–1 channel–1 with a high rejection of NaCl and KCl. This high water permeability,
which is about 50% of aquaporin Z’s capacity, makes channel 1 the fastest among the existing synthetic water channels
with high selectivity.
Modularly tunable monopeptidic scaffold enables rapid and combinatorial evolution of a halogen bond-mediated highly active chloride channel, exhibiting an excellent anticancer activity toward human breast cancer.
We
report here a unique ion-fishing mechanism as an alternative
to conventional carrier or channel mechanisms for mediating highly
efficient and exceptionally selective transmembrane K+ flux.
The molecular framework, underlying the fishing mechanism and comprising
a fishing rod, a fishing line and a fishing bait/hook, is simple yet
modularly modifiable. This feature enables rapid construction of a
series of molecular ion fishers with distinctively different ion transport
patterns. While more efficient ion transports are generally achieved
by using 18-crown-6 as the fishing bait/hook, ion transport selectivity
(K+/Na+) critically depends on the length of
the fishing line, with the most selective MF6-C14 exhibiting
exceptionally high selectivity (K+/Na+ = 18)
and high activity (EC
50 = 1.1 mol % relative
to lipid).
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.