Affiliation:
1. Ludwig-Maximilians-Universität München, Department für Pharmazie – Zentrum für Pharmaforschung
2. Bundeswehr Institute of Pharmacology and Toxicology
Abstract
A variety of 3,4-disubstituted pyridine derivatives with a tert-butyl group in the 4-position were synthesized in a transition-metal-free, two-step reaction sequence from 3-substituted pyridine precursors. Highly regioselective addition of t-Bu2Mg to TIPS-activated pyridines and an efficient microwave-assisted aromatization with sulfur as oxidant afforded the desired 3,4-disubstituted pyridine derivatives in moderate to excellent yields. The method is compatible with many functional groups such as ester, amide, halide, nitrile or alkyne groups present in the 3-position.
Funder
German Ministry of Defense
Subject
Organic Chemistry,Catalysis
Cited by
10 articles.
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