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  4. Regiochemical flexibility: the optional functionalization of 2,3,5-trihalopyridines at the 4- or 6-position
 
research article

Regiochemical flexibility: the optional functionalization of 2,3,5-trihalopyridines at the 4- or 6-position

Bobbio, Carla
•
Schlosser, Manfred  
2001
European Journal of Organic Chemistry

A deprotonation study was performed using 2,3,5-trichloropyridine, 3,5-dichloro-2-fluoropyridine, and 5-chloro-2,3-difluoropyridine as the substrates. Upon reaction with lithium diisopropylamide (LDA), deprotonation occurred exclusively at the 4-position. Subsequent carboxylation and iodination led to the acids and 4-iodopyridines. The exposure of the latter compds. to lithium 2,2,6,6-tetramethylpiperidide (LITMP) caused deprotonation and immediately ensuing iodine migration. The intermediates were trapped with dry ice to afford the carboxylic acids. Upon neutralization, the 6-iodopyridines were obtained. These compds. readily exchanged the heavy halogen for metal when treated with isopropylmagnesium chloride. In this way, functional groups could be selectively introduced in the 6-position. Employing carbon dioxide routinely as the model electrophile, trihalopyridinecarboxylic acids were formed which, all unknown so far, should provide valuable new building blocks for pharmaceutical research. Moreover, the selective nucleophilic displacement of the halogen at the 2-position could give rise to an immense variety of new structures. [on SciFinder (R)]

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Type
research article
DOI
10.1002/1099-0690(200112)2001:23%3C4533::AID-EJOC4533%3E3.0.CO;2-1
Author(s)
Bobbio, Carla
•
Schlosser, Manfred  
Date Issued

2001

Published in
European Journal of Organic Chemistry
Issue

23

Start page

4533

End page

4536

Subjects

Carboxylation; Iodination; Regiochemistry (functionalization of 2

•

3

•

5-trihalopyridines at the 4- or 6-position)

•

functionalization trihalopyridine; pyridine trihalo functionalization

Note

CAN 136:279303 27-16 Heterocyclic Compounds (One Hetero Atom) Section de Chimie (BCh),Universite de Lausanne,Lausanne,Switz. Journal 1434-193X written in English. 16063-70-0; 89402-43-7 Role: RCT (Reactant), RACT (Reactant or reagent) (functionalization of 2,3,5-trihalopyridines at the 4- or 6-position); 823-56-3P; 78121-76-3P; 406676-18-4P; 406676-19-5P; 406676-21-9P; 406676-23-1P; 406676-24-2P; 406676-26-4P; 406676-35-5P; 406676-37-7P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (functionalization of 2,3,5-trihalopyridines at the 4- or 6-position); 40360-44-9P; 406676-28-6P; 406676-30-0P; 406676-32-2P; 406676-39-9P; 406676-40-2P Role: SPN (Synthetic preparation), PREP (Preparation) (functionalization of 2,3,5-trihalopyridines at the 4- or 6-position)

Editorial or Peer reviewed

REVIEWED

Written at

EPFL

EPFL units
LSCO  
Available on Infoscience
March 3, 2006
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/226977
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