Parallel synthesis technologies

It was quickly realized that parallel synthesis techniques could be used to increase the efficiency of medicinal chemistry in this role [111]. Small optimization libraries were produced using parallel synthesis technologies and they took advantage of the ability... 

Parallel Synthesis Technologies in Lead Discovery and Optimization Strategies and Applications... 

Microwave and fluorous technologies have been combined in the solution phase parallel synthesis of 3-aminoimidazo[l,2-a]pyridines and -pyrazines [63]. The three-component condensation of a perfluorooctane-sulfonyl (Rfs = CgFiy) substituted benzaldehyde by microwave irradiation in a single-mode instrument at 150 °C for 10 min in CH2CI2 - MeOH in the presence of Sc(OTf)3 gave the imidazo-annulated heterocycles that could be purified by fluorous solid phase extraction (Scheme 9). Subsequent Pd-catalyzed cross-coupling reactions of the fluorous sulfonates with arylboronic acids or thiols gave biaryls or aryl sulfides, respectively, albeit it in relatively low yields. 

Parlow J. J. Flynn, D. L. Solution-Phase Parallel Synthesis of a Benzoxaz-inone Library Using Complementary Molecular Reactivity and Molecular Recognition (CMR/R) Purification Technology, Tetrahedron 1998,54,4013. 

P. Claus, M. Baerns, Parallel Synthesis and Fast Catalytic Testing of Heterogeneous Catalysis, Microreaction Technology Parallel Preparation and Testing of Catalysts, 21st June 2001, Dechema, Frankfurt/Main, Germany, Book of Abstracts. 

Manufacturing information systems for real-time process control in the lab and for efficient statistical process control, as well as the right number of lab trials, limits information losses between the plant and the labs. Parallel synthesis, such as units with online analytics in the lab, and the use of new technologies such as Micro Reaction Technology developed by Clariant and a few other companies for application in production mean a step change in reproducibility. 

Antonenko VV, Manual and automated parallel synthesis its development and application for drug discovery at Affymax-GlaxoWellcome, Presented at the First European Conference on Combinatorial Technologies, ComTech97, Freiburg, Germany, February 20-21, 1997. 

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