Combinatorial Chemistry & High Throughput Screening

Author(s): K. Cottrell, C. W. Holyoke, M. Kline, K. C. Lee, M. R. Nassirpour, R. J. Pasteris and S. Shah

DOI: 10.2174/138620705774575337

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Parallel, Solution Phase Synthesis of Dihydropyridine Miticides Via a Versatile Multicomponent Reaction

Page: [617 - 622] Pages: 6

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Abstract

A novel class of highly active dihydropyridine miticides was prepared using a multicomponent reaction process. The initial lead was rapidly optimized using solution phase parallel synthesis techniques and a positional scanning approach. Detailed structure-activity relationships were developed for the amino and carbonyl components of the molecule and used to select the best candidates for broad field testing. The chemistry, biology and toxicology of these compounds will be presented along with numerous structural variants of the reaction products.

Keywords: dihydropyridine, dihydropyrimidine, miticide, multicomponent reaction, parallel synthesis, 1,3-dinucleophile, 1,3 dielectrophile