Efficient Engineering and Production Concepts for Products in Regulated Environments – Dream or Nightmare?

Manufacturing of chemical‐pharmaceutical products is moving increasingly fast on a global scale. Therefore, developing and starting up production facilities fast, with high quality, and at reasonable costs has become extremely challenging. Engineering concepts like modularization, standardization and simultaneous/parallel engineering are discussed as methods for speeding up process design and filing for regulatory approval. Transfer from batch to continuous operation mode of production is pointed out as the key‐issue in such strategies.     

Textile research and development in the UK – success or failure?

Although initially lagging behind the USA, the amount and quality of research and development carried out in the UK can be compared favourably with that from other major world countries. The industrial research association, although a well‐conceived concept to increase research and development efforts that gave significant results, was disappointing for several reasons. A major problem has been the dissemination, exploitation and commercialisation of research results. The activities of research organisations need to be reviewed regularly, as they may have a relatively short lifespan. The intermediate research and technology sector, given adequate support, may be the vehicle for better utilisation of research and development results.     

Strategische Bioraffinerieprojekte in Deutschland – Was haben und was brauchen wir?

Biorefineries offer a high potential for economically attractive conversion of biomass, but some important questions concerning the implementation are unsolved. Different concepts for biorefineries are introduced     

Are 1,4‐ and 1,5‐Disubstituted 1,2,3‐Triazoles Good Pharmacophoric Groups?

Over the last decade, 1,2,3‐triazoles have received increasing attention in medicinal chemistry thanks to the discovery of the highly useful and widely applicable 1,3‐dipolar cycloaddition reaction between azides and alkynes (click chemistry) catalyzed by copper salts and ruthenium complexes. After a decade of medicinal chemistry research on 1,2,3‐triazoles, we feel that the time is ripe to demonstrate the real ability of this heterocycle to participate in important and pivotal binding interactions with biological targets while maintaining a good pharmacokinetic profile. In this study, we retrieved and analyzed X‐ray crystal structures of complexes between 1,2,3‐triazoles and either proteins or DNA to understand the pharmacophoric role of the triazole. Furthermore, the metabolic stability, the capacity to inhibit cytochromes, and the contribution of 1,2,3‐triazoles to the overall aqueous solubility of compounds containing them have been analyzed. This information should furnish fresh insight for medicinal chemists in the design of novel bioactive molecules that contain the triazole nucleus.     

Cyclobutanone Analogues of β‐Lactam Antibiotics: β‐Lactamase Inhibitors with Untapped Potential?

β‐Lactam antibiotics have been used for many years to treat bacterial infections. However the effective treatment of an increasing range of microbial infections is threatened by bacterial resistance to β‐lactams: the prolonged, widespread (and at times reckless) use of these drugs has spawned widespread resistance, which renders them ineffective against many bacterial strains. The cyclobutanone ring system is isosteric with β‐lactam: in cyclobutanone analogues, the eponymous cyclic amide is replaced with an all‐carbon ring, the amide N is substituted by a tertiary C?H α to a ketone. Cyclobutanone analogues of various β‐lactam antibiotics have been investigated over the last 35 years, initially as prospective antibiotics in their own right and inhibitors of the β‐lactamase enzymes that impart resistance to β‐lactams. More recently they have been tested as inhibitors of other serine proteases and as mechanistic probes of β‐lactam biosynthesis. Cyclobutanone analogues of the penam ring system are the first reversible inhibitors with moderate activity against all classes of β‐lactamase; other compounds from this family inhibit Streptomyces R61 dd ‐carboxypeptidase/transpeptidase, human neutrophil elastase and porcine pancreatic elastase. But has their potential as enzyme inhibitors been fully exploited? Challenges in synthesising diversely functionalised cyclobutanone derivatives mean that only a limited number have been made (with limited structural diversity) and evaluated. This review surveys the different synthetic approaches that have been taken to these compounds, the investigations made to evaluate their biological activity and prospects for future developments in this area.     

Neue Materialien – Was kann die Synthesechemie heute?

Materials of construction will exert a greater influence on cultural developments on all continents than in the past, meaning that research in materials science will have to be given a high interdisciplinary priority in countries with the right scientific and technological background. Particularly in the case of this developing area, science will have to emerge from its classical compartmentalization because further progress will require joint consideration of chemical, physical, and where appropriate biological aspects, while paying due attention to the creative scope of engineering. It will become more important than ever to combine science and engineering and to derive an innovative materials architecture from the more contemplative discipline of materials science.     

Diruthenium(I,I) Catalysts for the Formation of β‐ and γ‐Lactams via Carbenoid C?H Insertion of α‐Diazoacetamides

Intramolecular carbenoid C H insertion of five α‐diazoacetamides [N₂CH CONR₂, NR₂=NEt₂ ( 3a ), NBu₂ ( 3b ), N(i‐Pr)₂ ( 3c ), N(CH₂Ph)₂ ( 3d ), N(i‐Pr)(CH₂Ph) ( 3e )], was investigated using as catalysts dinuclear Ru(I,I) complexes of the type [Ru₂(μ‐L¹)₂(CO)₄L²₂], where L¹ is a bidentate bridging acetate, calix[4]arenedicarboxylate, saccharinate, pyridin‐2‐olate, or triazenide ligand, as well as [RuCl₂(p‐cymene)]₂. The Ru(I,I) complexes were found to be suitable catalysts for the carbenoid cyclization reactions, except in the case of 3a . With diazoamides 3b–e , [Ru₂(μ‐sac)₂(CO)₅]₂ (sac=saccharinate) and [Ru₂(μ‐6‐chloropyridin‐2‐olate)₂(CH₃CN)₂(CO)₄] are as effective as Rh₂(OAc)₄ under the same conditions, although some differences in the regioselectivity and chemoselectivity of the cyclization are observed. The carbenoid cyclization reactions yield γ‐lactams from diazoamides 3a and 3b , both a β‐ and a γ‐lactam from 3c , and a β‐lactam as well as a 3‐azabicyclo[5.3.0]deca‐5,7,9‐trien‐2‐one from 3d . With 3e , formation of γ‐lactam 21 and of bicyclic lactam 23 prevails.     

Biobasiertes Glycerin – ein neuer Rohstoff für die chemische Industrie?

Glycerol that originates as a by‐product from the production of biodiesel is a bio‐based feedstock, which neither has the disadvantages of fossil resources nor can be used as food. It was studied in a life cycle assessment whether a use in the chemical industry leads to environmental advantages. The life cycle assessment of options of use of glycerol from the biodiesel production shows that a conventional material use without conversion is the environmentally most advantageous option. However, it is to be expected that not all glycerol can be used this way if the biodiesel production increases. In this case, innovative biotechnological conversions of glycerol to n‐butanol or 1,3‐propanediol as well as the use for energy production can be environmentally advantageous if especially the energy and resource efficiencies are further optimized.     

Catalytic Membrane Reactors – Lab Curiosity or Key Enabling Technology?

Two industrially interesting partial oxidations have been performed in catalytic membrane reactors with oxygen‐transporting membrane: aromatization of natural gas and oxidation of ammonia to nitric oxide. In both reactions, the oxygen used has been separated from air through a perovskite membrane, which also is the catalyst for the ammonia oxidation. When conducting the methane aromatization in an oxygen‐transporting membrane reactor, coke deposition is reduced and the aromatics yield is higher than that of a reference non‐oxidative fixed‐bed reactor.