By Guillermo Morales, Barry A. Bunin
Combinatorial Chemistry encompasses either the layout of compounds for particular pharmacological use and the screening of molecules in excessive throughput automatic exams to discover energetic brokers with particular services.
*Direct sorting break up and pool combinatorial synthesis
*Linkers and their applications
*Microwave assisted synthesis
*Peptide Synthesis and Screening
*Polymer assisted approaches
*Small molecule and heterocycle synthesis
Read Online or Download Methods in Enzymology, Vol. 369: Combinatorial Chemistry, Part B PDF
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Additional info for Methods in Enzymology, Vol. 369: Combinatorial Chemistry, Part B
DNA-binding systems 69 consist of an oligosaccharide (A) selected to recognize a DNA sequence and a labile nine-membered enediyne moiety (B) that can generate a reactive diradical. These compounds were found to be difficult to handle in a previous solution phase synthesis due to the presence of both the water-soluble sugar (A) and the hydrophobic enediyne moiety (B). The oligosaccharide-trialkylsilyl linker system was prepared by solution phase synthesis and loaded onto SynPhase polystyrene Crowns to give 67 (Scheme 19).
Quality of the products 32 ranged from 56 to 99% purity with the average being 83%. 37 at Mimotopes developed a one-pot synthesis of benzimidazoles using chloromethylated SynPhase Lanterns functionalized with Wang linker (Scheme 11). The support-bound ester 33 was treated with aliphatic and aromatic amines to afford o-nitroanilines 34 with little, if any, premature cleavage. 75 M SnCl2Á2H2O (10 equivalents) in DMF and heating at 60 for 3 h. The support-bound products were readily cleaved from the Lanterns with 20% TFA/CH2Cl2 to afford the desired disubstituted benzimidazoles 36.
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