Monatshefle ftir Chemie 128, 697-700 (1997)
Monatshefte fib"Chemie
Chemical Monthlp
© Springer-Verlag 1997
Printed in Austria
On the Reaction Between Alkyl Isocyanides
and 3-Benzylidene-2,4-pentanedione.
A Convenient Synthetic Route to Densely
Functionalized Furans
I. Yavari*, A. Shaabani, and M. T. Maghsoodlou
Chemistry Department, Tarbiat Modarres University, Tehran, Iran
Summary. Alkyl isocyanides undergo a formal [1 ÷ 4] cycloaddition reaction with 3-benzylidene-
2,4-pentanedione yielding multiply functionalized furan ring systems in fairly high yields. The ]H
NMR spectrum of 4-acety1-2-(N-benzylamino)-5-methyl-3-pnenylfuran shows an AB pattern for the
benzylic methylene protons as a result of a restricted rotation about the bond between the acetyl
group and the furan ring, thus giving rise to perpendicular disymmetric planes.
Keywords. Alkyl isocyanides; [1 + 4] Cycloaddition; Conformational enantiomers; Functionalized
furan.
Eine einfache Synthese von hochfunktionalisierten Furanen durch Reaktion von
Alkylisocyaniden mit 3-Benzyliden-2,4-pentadion
Zusammenfassung. Alkylisocyanide gehen mit 3-Benzyliden-2,4-pentadion eine formale [1 + 4]-
Cycloaddition ein, die in relativ hohen Ausbeuten zu mehrfach funktionalisierten Furansystemen
ftihrt. Das 1H-NMR-Spektrum von 4-Acetyl-2-(N-benzylamino)-5-methyl-3-phenylfuranzeigt ftir
die benzylischen Methylenprotonen ein AB-System, da das Molektil durch die sterische Hinderung
der Rotation der Acetylgruppe asymmetrisch wird.
Introduction
Isocyanides [1-4] undergo a formal [1 + 4] cycloaddition reaction with conjugated
electrophilic heterodienes. These reactions are of interest for the synthesis of func-
tionalized heterocyclic five-membered ring systems. Cycloadditions of isocyanides
with azadienes [5], diazadienes [6], N-acylimines [7], o~, fl-unsaturated esters [81,
enones [9], and nitroalkenes [101 have been described.
We report herein that alkyl isocyanides (1) undergo smoothly a formal [1 + 4]
cycloaddition reaction with 3-benzytidene-2,4-pentanedione (2) [11], yielding N-
substituted 4-acetyl-2-alkylamino-5-methyl-3-phenyl furans (4).