|Scalability of Heterocyclic Microwave-Assisted Transformations From Batch to Continuous Flow - A Case Study|
Jennifer M. Kremsner, Bimbisar Desai, Alexander Stadler and C. Oliver Kappe
Herein we present a case study on the small to large scale microwave-assisted synthesis of the DHPM 4 under batch and continuous flow conditions in monomode and multimode cavities.
|High-Speed Transition Metal-Catalyzed Chemistry Promoted by Microwave Irradiation|
Toma Glasnov, Peter Walla, Alexandler Stadler, Alenka Lengar,Bimbisar Desai, Bogdan Khanetskyy, Doris Dallinger and C. Oliver Kappe
When using traditional heating under reflux conditions many transition metal-catalyzed C-C and C-X bond forming reactions typically need hours or days to reach completion. Fast and reliable microwave protocols are therefore very much needed for speeding up transformations in the field of homogeneous catalysis, taking into account the advantages of microwave heating – rapid transfer of energy and inverted temperature gradients, by increasing the lifetime of the catalyst, i.e. eliminating the wal
|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.