|Rapid Generation of Polymer-Bound Enones by Microwave-Assisted Solid-Phase-Synthesis|
Gernot A. Strohmeier and C. Oliver Kappe
We have shown that two important reactions in solid-phase synthesis can be easily accelerated by the assistance of microwave irradiation. Acetoacetylations were performed in 1-5 minutes instead of 18 hours. Knoevenagel condensations were acceptably reduced from 1-3 days to one hour. The increased temperatures didn’t reduce the purity of the final products.
|Microwave Assisted Synthesis of Substituted 2(1H)-Quinolones as Maxi-K+ Channel Openers|
Toma Glasnov, Wolfgang Stadlbauer and C. Oliver Kappe
Here we present a novel synthetic strategy for synthesis of 4-aryl-2(1H)-quinolone lead compounds for the treatment of male ED. The MW-reaction protocols are high-diversity generating, flexible, amenable to high-speed MAOS, scalable and involve commercially available building blocks. Our approach for making the 4-arylquinolones includes a cyclization step, chlorination/hydrolysis, Suzuki C-C coupling, bromination, and finally a Heck reaction, all under microwave conditions.
|Automated Generation of a Dihydropyrimidine Library Using Sequential Microwave-Assisted Synthesis|
Alexander Stadler and C. Oliver Kappe
The aim of this study was to generate a library of dihydropyrimidines utilizing rapid automated sequential microwave-assisted chemistry.
|Interfacing Microwave Synthesis with Enabling Technologies in Drug Discovery|
Doris Dallinger and C. Oliver Kappe
Here we report on the rapid synthesis/decoration of privileged heterocyclic scaffolds, namely the dihydropyrimidine (DHPM) scaffold, by applying microwave heating in conjunction with PASP approaches.
|Polymer-Bound Fused N -(1-Chloroalkyl)Azinium Chlorides As Synthetic Equivalents Of Aldehydes. |
Jean Jacques Vanden Eynde, Annie Mayence and Ernst Anders.
A few years ago the first multi-component synthesis of N-(1 -haloalkyl) pyridinium halides from a thionyl halide, pyridine, and an aldehyde was described. Since that time, we have widely demonstrated that such salts can be considered as valuable synthetic equivalents of the starting aldehydes for the preparation of various classes of nitrogen heterocycles.
|Application of Microarrays in Process Analytical Technologies A First Step Towards Real Time Product Release|
Streefland M, van de Waterbeemd B, vander Pol LA, Beuvery EC, Martens DE,Tramper J
Application of microarrays during process development helps to gain insight in biological processes involved in product formation, increasing process understanding.
|From Medicinal Plants to Bioactive Drugs|
Ilaria Lampronti, Mahmud T.H. Khan, Antoine M. Saab, Elisabetta Lambert, Letizia Penolazzi, Roberta Piva and Roberto Gambari
The aim of our study was to analyze the antiproliferative activity effects on human tumor cell lines and the differentiating activity on human erythroleukemic K562 cells of different extracts derived from medicinal plants of Bangladesh and Lebanon.
|Development of an Analytical Data Management System (ADMS) to Accelerate the Selection of a Suitable API Form Through Salt and Polymorph Screening|
Raeann Wu, Peter Karpinski, Patrick Drumm, Karim Kassam, Michel R.J. Hachey and Michael Boruta
In this work, we discuss the acceleration of the preformulation process through the use of modern software systems. The data system discussed can read, process, store, retrieve, visualize and report a wide variety of data type—XRD, Raman, HPLC, NMR, TGA, DSC, chemical structures, properties and images—in a centralized and homogeneous way. A pilot study at a pharmaceutical company demonstrated possible time savings between 20% and 80% at various points in the preformulation workflow.
|Exploring Reverse Transcription for DNA MicroArrays|
Miroslava Cuperlovic-Culf, Adrian S. Culf, Dominique Richard, Mark LaFlamme, Daniel Leger and Rodney J. Ouellette
Results suggest that random priming is the optimal method for expression analysis of long genes. This method of RT may be appropriate for alternatively spliced genes and for genes without unique probes in the 3’-region.