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Synthesis of medium sized ring by radical ipso-substitution

Synthesis of medium sized ring by radical ipso-substitution
Synthesis of medium sized ring by radical ipso-substitution

A new approach to seven, eight and nine membered ring synthesis involving a radical ipso-substitution is described.  The  method involves treatment of a 2-iodobenzyl-indanone or tetralone with tributyltin hydride and AIBN.  Addition of the resulting aryl radical to the pendant carbocycle then occurred in a 5-exo-trig manner to the ring junction.  Fragmentation of the resulting radical intermediate lead to rearomatisation of the arene and to the formation of a highly stabilised radical.

With tetralone derivatives the 5-exo-trig ipso-cyclisation completed with 6-endo/exo-ortho-addition while in the case of benzocyclobutane a competing 5-exo trig cyclisation to a nitrile was observed in addition to the formation of the seven membered ring.

A study on the use of tetrakistrimethylsilyl silane-TBAF for the reduction of the aryl halides is also presented.

University of Southampton
L'Hélias, Nathalie Sylvie
ae5ad565-bbc8-4385-bcff-e3ff1d4e92bb
L'Hélias, Nathalie Sylvie
ae5ad565-bbc8-4385-bcff-e3ff1d4e92bb

L'Hélias, Nathalie Sylvie (2005) Synthesis of medium sized ring by radical ipso-substitution. University of Southampton, Doctoral Thesis.

Record type: Thesis (Doctoral)

Abstract

A new approach to seven, eight and nine membered ring synthesis involving a radical ipso-substitution is described.  The  method involves treatment of a 2-iodobenzyl-indanone or tetralone with tributyltin hydride and AIBN.  Addition of the resulting aryl radical to the pendant carbocycle then occurred in a 5-exo-trig manner to the ring junction.  Fragmentation of the resulting radical intermediate lead to rearomatisation of the arene and to the formation of a highly stabilised radical.

With tetralone derivatives the 5-exo-trig ipso-cyclisation completed with 6-endo/exo-ortho-addition while in the case of benzocyclobutane a competing 5-exo trig cyclisation to a nitrile was observed in addition to the formation of the seven membered ring.

A study on the use of tetrakistrimethylsilyl silane-TBAF for the reduction of the aryl halides is also presented.

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Published date: 2005

Identifiers

Local EPrints ID: 465500
URI: http://eprints.soton.ac.uk/id/eprint/465500
PURE UUID: 31bbaf95-e042-4b2a-9f46-8f5d7ad5481d

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Date deposited: 05 Jul 2022 01:28
Last modified: 16 Mar 2024 20:13

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Author: Nathalie Sylvie L'Hélias

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