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  4. Switchable [3+2] and [4+2] Heteroannulation of Primary Propargylamines with Isonitriles to Imidazoles and 1,6-Dihydropyrimidines: Catalyst Loading Enabled Reaction Divergence
 
research article

Switchable [3+2] and [4+2] Heteroannulation of Primary Propargylamines with Isonitriles to Imidazoles and 1,6-Dihydropyrimidines: Catalyst Loading Enabled Reaction Divergence

Tong, Shuo  
•
Wang, Qian  
•
Wang, Mei-Xiang
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2016
Chemistry - A European Journal

Isonitrile 1 due to its carbene-like reactivity serves generally as a one-carbon synthon in a diverse set of organic transformations. We report in this article that the isocyano group can also act as a polarized triple bond to undergo, as a two-atom synthon, heteroannulation with primary propargylamines 15. In addition, we serendipitously discovered that the reaction pathways can be modulated by simply changing the catalyst loading. In the presence of 0.1 equiv of Yb(OTf)3 or TfOH, the reaction between 1 and 15 afforded exclusively imidazoles 16 by a formal [3+2] cycloaddition. At a higher catalyst loading (Yb(OTf)3 (0.4 equiv) or TfOH (0.5 equiv)) under otherwise identical conditions, the same reaction furnished 1,6-dihydropyrimidines 17 in good to excellent yields by way of a formal [4+2] cycloaddition process. Mechanistic investigations indicated that both annulations went through an amidine intermediate resulting from the insertion of the isocyano group to the NH bond of the primary amine. Subsequent catalyst-loading-dependent 5-exo-dig or 6-endo-dig cyclization provided selectively the two heterocycles, respectively.

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Type
research article
DOI
10.1002/chem.201601560
Web of Science ID

WOS:000380269400038

Author(s)
Tong, Shuo  
Wang, Qian  
Wang, Mei-Xiang
Zhu, Jieping  
Date Issued

2016

Publisher

Wiley-Blackwell

Published in
Chemistry - A European Journal
Volume

22

Issue

24

Start page

8332

End page

8338

Subjects

dihydropyrimidine

•

heteroannulation

•

imidazoles

•

insertion

•

isonitriles

•

propargylamine

Editorial or Peer reviewed

REVIEWED

Written at

EPFL

EPFL units
LSPN  
Available on Infoscience
June 9, 2016
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/126568
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