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  Volume: 27
Number: 2
Term: MAR/APR
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CONTENTS
EDITORIAL
DETACHABLE SUPPLEMENT ON ANALYTICAL TECHNOLOGIES
COVER STORY
MICROWAVES
PRODUCT FOCUS
MICROREACTORS
SUSTAINABILITY
PROCESS DEVELOPMENT
MEDICINAL CHEMISTRY
NEWS - SUPPLIERS & SERVICES
Towards peptide-based diagnostics
Authors: PAPINI A.M.
In the last years new perspectives in the development of in vitro diagnostics opened a future for more efficient and reliable technologies particularly to help the management of immune-mediated diseases not only autoimmune diseases, but also different cancer forms
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PRODUCT FOCUS - The future flows through Corning advanced-flow glass reactors. Engineered to move you to market faster and more efficiently
Authors: CORNING SAS (FRANCE)
Corning, leader in specialty glass, introduces its advanced-flow glass reactor, replacing conventional batch processing and lowering manufacturing costs. Corning reactors contain glass fluidic modules providing combined mixing, mass and heat transfer, and offer chemical resistance over a wide range of temperatures and pressures to perform multiphase and multistep applications. Reactors are parallelized to achieve the required production capacity, avoid scale-up issues and reduce time to market
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Microwave synthesis in process chemistry. Method, scale and scope
Authors: MOSELEY J.D. (AstraZeneca, UK)
This review will present the current state of commercial microwave scale-up instruments for organic synthesis in process chemistry within the context of the pharmaceutical industry. The different methods of scale-up will be discussed and the effect this has on the scale achievable. Representative examples of pharmaceutical chemistry will be given for each instrument type. Other applications of how microwave heating can aid the process development chemist will also be presented briefly
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Microwave-assisted palladium(II)-catalyzed heck reactions
Authors: LINDH J., LARHED M. (Uppsala University, SWEDEN)
During the last couple of years we have reported on a number of microwave promoted oxidative Heck reactions with the aim of developing efficient and environmentally benign procedures. The use of microwave irradiation has enabled us to drastically improve reaction rates and to use substrates which are virtually unreactive at lower temperatures
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CHEMTRIX
Authors: Chemtrix (NETHERLANDS)
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Synthesis of pharmaceutical and bio-active compounds in microreactors
Authors: MAK X.Y., LAURINO P., SEEBERGER P.H. (Swiss Federal Institute of Technology, SWITZERLAND)
Microreactor technology is beginning to find broad applications in organic synthesis. Here, some recent applications of continuous flow microreactors for the synthesis of pharmaceutically relevant intermediates and scaffold systems will be discussed using specific syntheses as examples. Some of the key advantages offered by the use of these miniaturized devices are highlighted
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Carbon dioxide. A C-1 source for chemical industry
Authors: CAGLIOTI L., MICSKEI K., TACCONI L., ZUCCHI C. ET ALL (Univ La Sapienza, ITALY)
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
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Catalytic asymmetric hydrogenation of enamides. Problems and challenges on scale
Authors: SINGH S.P., KOENIG S.G., WAGLER T.R. (Sepracor, USA)
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
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A Review on membrane crystallization
Authors: DI PROFIO G., CURCIO E., DRIOLI E. (Univ of Calabria, ITALY)
The opportunity to couple membrane processes and crystallization operations, 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
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Design and implementation of a fragment discovery platform
Authors: BARKER J.J., FELICETTI B., HESTERKAMP T., WHITTAKER M. (Evotec, UK)
Fragment-Based Drug Discovery is increasingly being utilized to tackle both routine pharmaceutical targets as well as more demanding targets which may have previously proven problematic to traditional drug discovery techniques. Successful Fragment-Based Drug Discovery requires the integration of diverse techniques to deliver an efficient and effective platform for rapid advances in drug discovery. This article describes the components of a fragment discovery platform which when combine deliver an effective method for hit finding and rapid progression into drug discovery
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Exploration of chemical space for drug discovery by database generation
Authors: REYMOND J.L., NGUYEN K.T. (Univ of Berne, SWITZERLAND)
Small molecule drug discovery requires constant innovation The exhaustive enumeration of the 26.4 million possible small organic molecules up to 11 atoms of C, N, O, F in the database GDB shows that 99.8 percent of the small molecule chemical space has yet to be explored. Guided by virtual screening tools, a proof-of-principle study shows that novel bioactive ligands from GBD can be readily identified. As an example, inhibitors of the NMDA-receptor glycine site, an important CNS target, are described.
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