Isopropenyl acetate: A cheap and general acylating agent of alcohols under metal-free conditions

Functionalized primary, secondary and tertiary alcohols are efficiently acetylated by isopropenyl acetate and catalytic p-TsOH.     

Synthetic Communication: Synthesis of Optically Pure Analogues of D-Arginine Methyl Ester with Antiarrhythmic Activity

The synthesis of the methyl esters of optically pure trans and cis 4-guanidinocyclohexylglycine as rigid analogues of D-arginine methyl ester are described.     

Native and polymeric β-cyclodextrins in performance improvement of chitosan films aimed for buccal delivery of poorly soluble drugs

β-Cyclodextrin (βCD) and its soluble polymeric derivative (EPIβCD) were used to improve the effectiveness of chitosan-based bucco-adhesive film formulations containing bupivacaine hydrochloride and triclosan as poorly-soluble model drugs. The film formulations were characterized in terms of swelling, mucoadhesion and in vitro drug release, while possible interactions between the components were investigated by DSC and FTIR analyses. For both drugs EPIβCD showed a higher solubilizing efficiency than βCD; however cyclodextrin effectiveness in improving the release rate from film formulations was influenced by their different interactions with chitosan. Free βCD acted as a channelling agent, favouring the film swelling, while EPIβCD due to interaction with chitosan caused an opposite effect. βCD was the optimal partner for bupivacaine-loaded films in terms of film swelling, mucoadhesion and drug release. Contrariwise, EPIβCD was the best partner for triclosan-loaded films, allowing the highest drug release rate increase, due to its higher solubilizing ability with respect to βCD. Addition of the suitable cyclodextrin enabled formulation of buccal films with suitable drug release properties.     

Revenue Models and Policies for the Car Rental Industry

In this paper, we consider the application of revenue management techniques in the context of the car rental industry. In particular, the paper presents a dynamic programming formulation for the problem of assigning cars of several categories to different segments of customers, with rental requests arising dynamically and randomly with time. Customers make a rental request for a given type of car, for a given number of days at a given pickup time. The rental firm can satisfy the demand for a given product with either the product requested or with a car of at most one category superior to that initially required, in this case an “upgrade” can take place. The one-way rental scenario, which allows the possibility of the rental starting and ending at different locations, is also addressed. In the framework considered, the logistic operator has to decide whether to accept or reject a rental request. Since the proposed dynamic programming formulations are impractical due to the curse of dimensionality, linear programming approximations are used to derive revenue management decision policies for the operator. Indeed, primal and dual acceptance policies are developed (i.e. booking limits, bid prices) and their effectiveness is assessed on the basis of an extensive computational phase.     

Polymerization-Driven Photoluminescence in Alkanolamine-Based C-Dots

Carbonized polymer dots (CPDs), a peculiar type of carbon dots, show extremely high quantum yields, making them very attractive nanostructures for application in optics and biophotonics. The origin of the strong photoluminescence of CPDs resides in a complicated interplay of several radiative mechanisms. To understand the correlation between CPD processing and properties, the early stage formation of carbonized polymer dots has been studied. In the synthesis, citric acid monohydrate and 2-amino-2-(hydroxymethyl)propane-1,3-diol have been thermally degraded at 180 °C. The use of an oil bath instead of a more traditional hydrothermal reactor has allowed the CPD properties to be monitored at different reactions times. Transmission electron microscopy, time-resolved photoluminescence, nuclear magnetic resonance, infrared, and Raman spectroscopy have revealed the formation of polymeric species with amide and ester bonds. Quantum chemistry calculations have been employed to investigate the origin of CPD electronic transitions. At short reaction times, amorphous C-dots with 80 % quantum yield, have been obtained.     

Magneto-responsive nanocomposites: Preparation and integration of magnetic nanoparticles into films,capsules, and gels

This review reports on the latest developments in the field of magnetic nanocomposites, with a special focus on the potentials introduced by the incorporation of magnetic nanoparticles into polymer and supramolecular matrices. The general notions and the state of the art of nanocomposite materials are summarized and the results reported in the literature over the last decade on magnetically responsive films, capsules and gels are reviewed. The most promising concepts that have inspired the design of magneto-responsive nanocomposites are illustrated through remarkable examples where the integration of magnetic nanoparticles into organic architectures has successfully taken to the development of responsive multifunctional materials.     

Design,Synthesis, and Biochemical Evaluation of Alpha-Amanitin Derivatives Containing Analogs of the trans-Hydroxyproline Residue for Potential Use in Antibody-Drug Conjugates

Alpha-amanitin, an extremely toxic bicyclic octapeptide extracted from the death-cap mushroom, Amanita phalloides, is a highly selective allosteric inhibitor of RNA polymerase II. Following on growing interest in using this toxin as a payload in antibody-drug conjugates, herein we report the synthesis and biochemical evaluation of several new derivatives of this toxin to probe the role of the trans-hydroxyproline (Hyp), which is known to be critical for toxicity. This structure activity relationship (SAR) study represents the first of its kind to use various Hyp-analogs to alter the conformational and H-bonding properties of Hyp in amanitin.