Abstract: We discuss a peptide that targets cells in the acidic tissues that result from a range of pathological states, including tumours, and that can also translocate cell-impermeable cargo molecules across cell membranes in a pH-dependent manner. The technology is based on the interactions of a water-soluble membrane peptide, which we call pHLIP (pH (Low) Insertion Peptide), with the lipid bilayers of cell membranes. at the normal pH of healthy tissue it binds to cell surfaces, but at low pH pHLIP inserts as a monomer across the cell membrane to form a stable transmembrane helix. pHLIP holds promise for imaging and drug delivery applications.

Abstract: DSM as manufacturer of fine chemicals and active pharmaceutical ingredients and Corning Incorporated as manufacturer of modular micro-structured flow-through reactors have collaborated to develop and pilot a new process to perform a selective nitration under cGMP conditions. Nitration reactions are difficult to handle due to the exothermic properties of organic nitrates. In order to achieve high selectivity, classically high dilution conditions are used. DSM developed and intensified a process to utilize the capabilities of the Corning's reactor technology, combining the advantages of the micro-structured devices with extraction equipment. This combination has resulted in a highly efficient process, which was quickly and easily transferred from the laboratory to production, resulting in the processing of more than 25 metric tons of material and in the production of more than 0.5 metric tons of the desired quality product under cGMP conditions.

Abstract: Biocides are used in a wide range of applications and yet public information on their extent of use, efficacy and mechanisms of bacterial interactions is scarce. A number of academic studies have reported the possibility of emerging bacterial resistance following biocide exposure, and highlighted the occurrence of cross-resistance between unrelated antimicrobial agents such as biocides and chemotherapeutic antibiotics. A number of biocide-resistance mechanisms have been described at the bacterial cell and population levels. However, concrete evidence of emerging resistance in vivo is lacking because too few studies have been commissioned. Likewise, there is no consensus yet on the methodologies to be used to study bacterial resistance. Such protocols are urgently needed to provide an appropriate risk assessment on the use of these antimicrobial products

Abstract: Flow reactors with millimetric internal dimensions, to which Corning ® Advanced-Flow ™ glass reactors belong, are a proven technology which enables the switch from batch mode to continuous processing of chemical reactions. This results in more economical, efficient and safer processes. These reactors can be used from development to production. An efficient scale-up, complementary to numberin up, is obtained by increasing channel height or / and the footprint and internally dividing the flow. The effects of both approaches on a specific design are presented. The solution proposed ― higher footprint and internal split ― shows comparable pressure drop, emulsion quality and residence time distribution with better heat transfer at equivalent residence times. These good performances achieved in scaled-up Advanced-Flow ™ reactors enable the increase of overall production without altering the productivity achieved at lower scale.

Abstract: Esters of cellulose and starch are well known commercial materials. Cellulose acetate, for example, is a major product with annual global production of over 1.5 billion pounds. The conventional acetylation processes involve solvents such as methylene chloride or high temperature with sulfuric or perchloric acid as a catalyst. A review is provided here of the recent reports concerning rapid, alternative preparation of cellulose and starch esters. The process entails reaction of the cellulose or starch with acetic anhydride in the presence of a catalytic level of iodine, and in the absence of additional solvents. The reactant stoichiometry, reaction temperature, and reaction time all have effects on the degree of substitution of the ester and the reaction yield. Included in the review are the proposed modes of action for iodine, the mechanism, and assessment of the utility of this approach.

Abstract: Following pre-registrations, companies are required to cooperate in the relevant SIEF (s), which represents a real challenge, especially for SIEFs with hundreds of participants. Efforts are underway to organise such cooperation and many companies have opted to form or join consortia. The main weakness of REACH consortia agreements in place is that they are designed for situations where all SIEF participants are members of the relevant consortium, which is not the case with the vast majority of the SIEFs. The lack of appropriate rules for consortia relationship with other SIEF participants may affect their efficient functioning and lead to legal disputes. In this article, the authors give a description of the main features of the REACH consortia agreements and of the issue arising, with focus on relationship with other SIEF participants.

Abstract: IPEC has published Qualification of Excipients for Use in Pharmaceuticals detailing processes for developing and sourcing excipients and discusses issues that must be resolved for development of a commercial agreement. The document is divided into the Excipient Supplier's Process, the Users Process, and concludes with the Negotiation Process. The guideline provides a framework for suppliers and users of excipients to better understand the barriers to the introduction of new excipients and alternate sources of existing excipient grades. This dialogue provides for easier resolution of technical, safety, and regulatory issues concerning excipients. in December 2008, IPEC published Qualification of Excipients for Use in Pharmaceuticals. This guide of international applicability details processes for developing and sourcing excipients from the perspective of both the excipient supplier and user and provides a discussion of the issues that must be resolved to allow for development of a commercial agreement between the two parties. This article presents an overview/summary of the IPEC guide. IPEC is an international industry association formed in 1991 by manufacturers and end-users of excipients. It is an association comprising four regional pharmaceutical excipient industry associations covering North America, Europe, China and Japan (which are known respectively as IPEC-Americas, IPEC Europe, IPEC-China and JPEC). IPEC's objective is to contribute to the development and harmonisation of international excipient standards, the introduction of useful new excipients to the marketplace, and the development of best practice and guidance concerning excipients.

Abstract: The enantiomers of 2-azabicyclo[2.2.1]hept-5-en-3- one are extremely versatile synthons and are being used in a growing number of drug candidates. A number of years ago we discovered a bioresolution approach to these compounds utilising a lactamase catalysed resolution of the racemic material. Discovery of efficient enzymes from wild type strains with complementary stereoselectivity made synthesis of both isomers of 2-azabicyclo[2.2.1]hept-5-en-3-one possible. These processes have been further developed throughout the years and remain the most efficient approach to prepare synthons of this type. This paper describes the development of the lactamase enzymes and exemplifies the growing applicability of synthons derived from (+)- and (-)-2-azabicyclo[2.2.1]hept-5- en-3-one.

Abstract: Asymmetric autocatalysis (i.e. enantioselective autocatalysis) with amplification of enantiomeric excess is found in the enantioselective addition of diisopropylzinc to pyrimidine-5-carbaldehyde using pyrimidyl alkanol as an asymmetric autocatalyst. Pyrimidyl alkanol with extremely low enantiomeric excess automultiplies during three consecutive asymmetric autocatalyses with significant amplification of enantiomeric excess up to > 99.5 percent ee. The asymmetric outocotolysis has been applied to chiral discrimination of cryptochiral compounds. It also provides clues for clarifying the origin of homochirality. Circularly polarized light, inorganic chiral crystals, chiral crystals of achiral organic compounds and chiral compounds resulting from carbon isotope substitution act as chiral initiators in asymmetric autocatalysis affording highly enantioenriched products. Asymmetric autocatalysis in the reaction between pyrimidine-5-carboldehyde and diisopropylzinc has enormous power to amplify the statistically induced tiny enantiomeric imbalance (fluctuation of ee), thus, it is possible to form large amount of optically active compounds without the use of any chiral material. Spontaneous absolute asymmetric synthesis has been realized for the first time.

Abstract: The application of flow reactors to increase the parameter space of organic chemistry reactions in current laboratory practice is explored. Using examples such as DielsAlder reactions, Knorr reactions and others, the paper demonstrates the advantages of flow reactors operating in a parameter space up to 350°C (662°F) and 200 bar (2900 psi), sometimes under supercritical conditions, and in some cases without catalysts. The flow reactors described in the paper offer for the first time an alternative solution to the microwave batch scale up.

Abstract: Multiphase hydrogenation using heterogeneous catalyst was conducted in a glass continuous flow reactor from Corning at the Centre for Process Innovation. The effect of temperature, hydrogen molar ratio, residence time, catalyst content and concentration were studied using noble-metal slurry catalyst. Efficient heat and mass transfer allow achieving full conversion with residence time lower than 1 minute and reduced catalyst load, while keeping selectivity in the same range as batch processes. These results show the high potential of Corning ® Advanced-Flow™ reactors for multiphase hydrogenations for high volume manufacturing.

Abstract: Current trends in the development of microstructured reactors with thin catalytic films (from 100 nm up to several microns) that have self-assembled nanostructures are discussed. A major technique that is used to prepare such films is sol-gel processing. This involves depositing a complex fluid on a microstructured substrate by dip, spin, or spray coating, followed by surfactant removal to form the porous nanostructures. A novel methodology has been developed by which a uniform coating containing controlled amounts of (poly)metallic nanoparticles can be obtained. This elegant strategy is based on the condensation of metal oxide species by self-assembly in the presence of metallic colloids. The potential microreactor applications brought forth by this innovative protocol are placed in perspective in the light of its versatility.

Abstract: The opportunity to couple membrane processes and crystallization, in order to develop an efficient crystallization technology, has been proposed in the form of a membrane crystallizer (MCr). In this system the membrane does not act simply as support for solvent evaporation, but also as a synthetic hydrophobic and porous surface able to activate heterogeneous nucleation starting at low super saturation and enhancing the kinetics of crystallization, even for large molecules like proteins. Thank to these advantages crystals with controlled morphologies and structures can be produced. Moreover, membrane crystallizers represent an additional option for realizing integrated and high efficient systems, operating in the logic of the process intensification strategy, to substantially improve in terms of water quahty, product recovery factor, overall cost, and environmental impact of brine, seawater desalination processes.

Abstract: Recent developments in the synthesis and uses of the primary synthons, SF 5 X (X = Cl, Br, SF 5 , C=CH, C 6 H 5 , (CF 2 ) n C 6 H 5 ) are discussed.

Abstract: The immense and increasing quantity of carbon dioxide in the terrestrial atmosphere could represent a rich resource of a C-1 reagent for chemical industry. The most serious problem with this raw material is the difficulty of its activation. This could be overcome by high energy investment (mostly: by light through photosynthetic biomass) or by suitable activating reagent. The latter possibility is now exploited by several suitable reactions. A few of these transformations are already industrialized. The main goal of the present paper is to help focusing attention on existing and potential possibilities of CO 2 chemistry, which could grow out as a serious and economic contribution to attempts at controlling climate change problems.

Abstract: Various perfluoro-2-methylene-1,3-dioxolanes substituted on 4 and 5 positions were synthesized from corresponding hydrocarbon precursors by direct fluorination in fluorinated solvent by F 2 / N 2 mixture. These perfluorodioxolane monomers were readily polymerized in bulk at 60-80°C using a perfluoroperoxide as the free radical initiator. The polymers obtained are completely amorphous. The refractive indexes and the glass transition temperatures are in the range of 1.3280 ~ 1.3570 at 632 nm and 90-185°C, respectively. They exhibit extraordinary optical transmittance from UV to near IR. They are chemically as well as thermally stable. The polymer obtained from perfluoro-2-methylene-1,3-dioxolane (without substitute on 4 and 5 position) was semi crystalline and melted at 230°C. However, when the crystalline powder was heated above the melting temperature and pressed, it became an amorphous transparent and flexible film and did not recrystallize below the glass transition temperature (110°C). The copolymers of these perfluorodioxolane monomers are also readily prepared in the solution or in bulk. The copolymers have only one T g from 110 to 165°C depending on the copolymer composition. The films prepared by casting were flexible and tough and had high optical transparency. The perfluorodioxolane polymers synthesized have extraordinary properties similar to commercially available perfluoropolymers such as Teflon AF ® , Hyflon AD ® and Cytop ® , and may have a wide range of applications in advanced optical and electronic technologies.

Abstract: Based on bibliometric analysis, this paper explores China’s publication activity in chemistry. China develops fast in chemical research and has taken a leading position in publishing journal papers. International collaboration plays a role in the Chinese chemical community, but this role varies among subfields.

Abstract: The applicability of ruthenium-indenylidene complexes in olefin metathesis polymerisations, in particular in ring opening metathesis polymerisation is discussed in this report. An indenylidene based alternative to state of the art initiators is introduced and the scope of this compound is discussed by means of application in block copolymer synthesis.

Abstract: The preparation of large amounts of recombinant protein is a major bottleneck for many areas of scientific research, including structural proteomics and therapeutic drug discovery. Recently the Small Ubiquitin-like Modifier (SUMO)-based fusion tag technology has gained increasing use for the expression of recombinant proteins. In E. coli recombinant proteins expressed as SUMO fusions have demonstrated enhanced stability and solubility, leading to greatly increased yields (5 to 20-fold) over constructs lacking this tag. Furthermore, efficient removal of the SUMO tag by SUMO protease allows the generation of a native N-terminus of the target protein. The use of SUMO-fusion technology in E. coli, termed SUMOpro, as well as the use of SUMOstar, an adaptation of SUMO for use in eukaryotic hosts, will be reviewed. This review will also provide a comparison between SUMOpro technology and other fusion tags commonly used to enhance protein production and facilitate purification.

Abstract: A nanocomposite of poly(propylene imine) dendrimer (PPI) and gold nonoparticle (AuNP) was prepared by cyclic voltammetric co-deposition on a screen printed carbon electrode (SPCE) and used as a platform for an electrochemical DNA nanobiosensor. The average size of the nanocomposite was <100 nm, with PPI clustering around AuNPs. Electrochemical impedance spectroscopy (EIS) measurements indicated that the dendrimeric gold nanoplatform markedly improved the conductivity andgresponse of the DNA biosensor, and gave a very low detection limit of 3 x 10 -10 M.

Abstract: This perspective presents an overview of waste-to-energy (WTE) incineration in China, outlining the demand for municipal solid waste (MSW) incineration, the development of WTE, and the control of air pollution from waste incineration; it also gives an outlook on WTE in addressing China's MSW disposal and supplying clean energy. Incineration is currently the second most important way of MSW management in China. Emissions of air pollutants from WTE facilities, including particulate matters, acidic gases, heavy metals, and dioxins, are low and meet the national emission standards. Besides reducing the volume of waste requiring landfill disposal, WTE can play a small but not insignificant role in electricity generation. Significant growth of WTE industry in China is expected in the next decade.

Abstract: Focussing its' research on illustrating the potential of continuous flow reactors to enhance chemical synthesis, the micro reactor group at The University of Hull has spent the past nine years developing continuous processes for an array of common synthetic reactions, enabling advantages such as reduced reaction times, enhanced reaction selectivity and increased yield to be highlighted. Using these observations as a starting point, recent studies have centred on increasing reaction complexity through the incorporation of solid-supported reagents, catalysts and biocatalysts into the flow reactors along with targeting the technology towards niche applications such as isotopic labelling.

Abstract: Achieving sustainability requires balancing economic, environmental, and social aspects. The awareness of and interest in sustainability are growing but the main question still remains unanswered: what economic and industrial activities could be considered sustainable and how could progress toward sustainability be measured? This article looks into the subject of measuring sustainability using a life cycle approach. To illustrate its application, two examples are considered, one related to energy and another to food. The article demonstrates how the results of sustainability measurement could help industry and consumers to identify more sustainable options.

Abstract: This article illustrates the application of catalytic asymmetric hydrogenation of enamides in the large-scale synthesis of trans-norsertraline. Problems and challenges encountered during the development and scale-up of the process, as well as their resolution, are highlighted. Specifically, the efficient synthesis of enamide and the hydrolysis of resulting acetamide were recognized as major issues in the application of this powerful technology for the development of large-scale chemical processes to chiral amines.

Abstract: Biocatalysts have significant potential for use in synthetic strategies to commercially important compounds due to their ability to perform highly stereoselective conversions. In addition, developments in protein and pathway engineering have led to biocatalyst improvements, enabled applications using non-natural substrates and alternative reaction stereoselectivities have been observed. An integrated multidisciplinary approach has been undertaken at UCL in the Departments of Chemistry, Biochemical Engineering and Structural and Molecular Biology (BiCE programme) focusing on biocatalytic approaches to ketodiols and aminodiols. This has led to the discovery of a new chemical reaction and colorimetric and chiral assays, and incorporated directed evolution strategies, targeted library formation, microwell miniaturization studies and whole process modelling.

Abstract: Widely used in various biomedical applications, aptamers are single-stranded DNA or RNA molecules with high specificiiy and binding affinity to the target molecules, which can be ascribed to their selection by an in vitro process, known as SELEX (systematic evolution of ligands by exponential enrichment). More specifically, cell-based SELEX, which uses whole disease cells as targets, can also produce aptamer probes that effectively differentiate cancer cells from healthy cells. Based on these properties, molecular assemblies can be rationally designed and engineered to fulfil many therapeutic objectives. Therefore in this review, we describe the most Important strategies for the molecular assembly of aptamer- conjugates, including those that involve aptamers, drugs, photosensitizers, and nanoparticles for use in regulating protein function, targeted drug delivery and cancer therapy. Their affinity and specificity to virtually any given protein make it possible to develop aptamers which can inhibit the activity of many pathogenic proteins in the clinic. In this review, we describe different strategies for molecular assembly of aptamers for use as antidotes in regulating protein function. The rational design of aptamers for targeted drug delivery and cancer therapy will also be discussed.

Abstract: The search for and development of non-fuel industrial uses of agricultural commodities is an ongoing endeavour. New technologies which can involve chemically, enzymatic ally, or genetically modifying agricultural products will be required in order meet the requirements of the products of the future, and to continue the eventual switch to an economy based on renewable resources. Adhesives, lubricants, polymers, and inks are some of the industries where we may see even more petrochemical replacement in the near future.

Abstract: This review discusses the recent development of highly active well-defined heterogeneous alkene metathesis catalysts based silica supported d 0 metal alkylidene complexes, which has led to advances in both homogeneous and heterogeneous catalyses. In particular, the high performances of the silica supported catalysts have several origins: the increase stability of reactive intermediates through site isolation on surfaces and the dissymmetry at the metal centre. These concepts are now being exploited to develop efficient homogeneous and heterogeneous csatalysts. Nonetheless, same key challenges still lie ahead such as stopping deactivation and finding regeneration processes.