What is it about?
The modified Sonogashira alkynone synthesis and the Bagley-Bohlmann-Rahtz pyridine synthesis can be consecutively combined in a one-pot fashion to give tri- and tetrasubstituted pyridines in a one pot fashion. With these processes 15 differently substituted 3-ethoxycarbonyl 2-methylpyridines can be readily obtained in modest to moderate yields.
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Why is it important?
Tri- and tetrasubstituted pyridines are important fragments in biologically active lead structures and pyridines per se are electron deficient heterocycles for application in life and materials sciences. Therefore, operatively straight forward one-pot synthesis for varying the pyrdines' substitution patterns are highly desirable.
Perspectives
The synthetic principle can be readily employed to create substance libraries for exploring the structure-porperty relationships and thereby optimizing the properties and performance of functional molecules.
Professor Thomas J J Müller
Heinrich-Heine-Universitat Dusseldorf
Read the Original
This page is a summary of: Consecutive three- and four-component coupling-Bagley-Bohlmann-Rahtz syntheses of tri- and tetrasubstituted pyridines, Zeitschrift für Naturforschung B, June 2016, De Gruyter,
DOI: 10.1515/znb-2016-0046.
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