Continuous Synthesis of a Macrocyclic Sulfite of Polyethylene Glycol by Cascaded Continuous Stirred Tank Reactors (CSTRs).

Invited for the cover of this issue is the group of Long Pan and co-workers at Asymchem Life Sciences (Tianjin) Co. Ltd. The image depicts a novel continuous process for the synthesis of a macrocyclic poly(ethylene glycol) (PEG) sulfite, the precursor to PEG macrocyclic sulfate, a useful building block in PEG chemistry. Read the full text of the article at 10.1002/chem.202304319.

Continuous Synthesis of a Macrocyclic Sulfite of Polyethylene Glycol by Cascaded Continuous Stirred Tank Reactors (CSTRs).

Many macrocyclic compounds are attractive drug-like molecules or intermediates due to their special properties. However, the bulk synthesis of such compounds are hindered by the necessity of using diluted solutions, in order to prevent intermolecular reactions that yields oligomer impurities, thereby resulting in a low production efficiency. Such challenge can be adequately addressed by using continuous reactors, allowing improved efficiency with smaller space footprints. In this work, we proposed a novel continuous process for the synthesis of a macrocyclic sulfite of tetraethylene glycol (PEG4-MCSi), which is a precursor to a very useful building block, PEG4-macrocyclic sulfate (PEG4-MCS). The basic reaction parameters, including stoichiometry and temperature, were first confirmed with small batch reactions, and the effectiveness of coiled reactors and continuous stirred tank reactors (CSTRs) were compared. Cascaded CSTRs were proven to be suitable, and the reaction parameters were subject to further optimization to give a robust continuous process. The process was then tested with 4 parallel runs for up to 64 h. Finally, the merits and demerits of batch and continuous reactions were also compared, demonstrating the suitability of latter in the bulk production of macrocyclic PEG-MCSi compounds.

Hydrogel Paint.

For a hydrogel coating on a substrate to be stable, covalent bonds polymerize monomer units into polymer chains, crosslink the polymer chains into a polymer network, and interlink the polymer network to the substrate. The three processes-polymerization, crosslinking, and interlinking-usually concur. This concurrency hinders widespread applications of hydrogel coatings. Here a principle is described to create hydrogel paints that decouple polymerization from crosslinking and interlinking. Like a common paint, a hydrogel paint divides the labor between the paint maker and the paint user. The paint maker formulates the hydrogel paint by copolymerizing monomer units and coupling agents into polymer chains, but does not crosslink them. The paint user applies the paint on various materials (elastomer, plastic, glass, ceramic, or metal), and by various operations (brush, cast, dip, spin, or spray). During cure, the coupling agents crosslink the polymer chains into a network and interlink the polymer network to the substrate. As an example, hydrogels with thickness in the range of 2-20 µm are dip coated on medical nitinol wires. The coated wires reduce friction by eightfold, and remain stable over 50 test cycles. Also demonstrated are several proof-of-concept applications, including stimuli-responsive structures and antifouling model boats.

Preliminary report of a new type of braided vein stent in animals.

BACKGROUND: Iliofemoral vein stenosis or occlusion is a common cause of severe chronic venous insufficiency. Endovascular venous stenting has become a preferred treatment because it is minimally invasive and has a high safety profile. Despite the wide application of the wallstent, it is not specifically designed for veins. There are currently few studies on braided stents in the field of veins. We designed a novel braided vein stent, which has higher radial resistive force and more optimized looped ends structure compared with the wallstent. The purpose of this study was to evaluate the safety and performance of the stent in animals, providing a reference for further clinical trials. METHODS: The Wallstent is used as a control group. The novel stent and the Wallstent were implanted in the iliac vein of sheep. After 30 days and 90 days, vascular injury, thrombus, neointima coverage, and luminal stenosis were evaluated through venous angiography, endoscopic observation of stent specimen and histopathology. Imaging, histology, and integration data were analyzed by t-test for comparisons between the groups. RESULTS: Two groups of stents were successfully implanted. Follow-up observation showed that there was no thrombosis or obstruction >50% occurred in any group and no significant differences in patency, vascular injury, or intimal hyperplasia compared with the Wallstent. CONCLUSION: The novel stent significantly increases the radial resistive force and does not increase vascular injury, thrombus and stent stenosis during 30-day and 90-day follow-up. The next step is to further validate the effectiveness of the stent through long-term animal observation and human clinical trials.

Lateral Extension of a Benzodithiophene System: Construction of Heteroacenes Containing Various Chalcogens.

A series of linear acenes with five fused rings, which contain thiophene, selenophene, and tellurophene as the outmost rings, have been synthesized from well-known benzodithiophene (BDT). It was found that the optical, electrochemical properties and crystal packing motifs could be modulated by changing heteroatoms in the outmost rings.