Issue in Honor of Prof. James Bull ARKIVOC 2002 (ix) 55-61
ISSN 1424-6376 Page 55
©
ARKAT USA, Inc
Unusual expressions of Michael reactivity of
1,3-bis(phenylsulfonyl)allene
James R. Bull, Nicholas S. Desmond-Smith, Steven J. Heggie, Roger Hunter,*
and Sophie C. M. Rees-Jones
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa
E-mail: roger@science.uct.ac.za
Dedicated to Professor James Ronald Bull on occasion of his retirement as Mally Professor
of Organic Chemistry at the University of Cape Town
Abstract: An improved procedure for producing the potent cycloaddition dienophile 1,3-
bis(phenylsulfonyl)allene 1 is described based on ensuring removal of excess triethylamine in the
work-up of the final dehydroiodination step. Triethylamine, as well as other tertiary amines,
promote trimerisation of 1 to 3 (X-ray shown), and a possible mechanism involving potentiation
via a Michael addition to 1 is proposed. A further expression of the potent Michael acceptor
character of 1 is provided by insertion into the α-position of THF to form 5. Mechanistically, this
is suggested as proceeding via an oxonium-ion ylide, also generated via initial Michael addition
of THF to 1.
Keywords: Michael addition, electrophilic allene, oxonium-ion ylide, α-insertion
Introduction
We have recently reported the synthesis of 1,3-bis(phenylsulfonyl)allene 1 and its application as
a useful dienophile in Diels-Alder reactions.
1
During development of its chemistry, several
unusual facets of reactivity were noted based on its ability to act as a potent Michael acceptor.
This paper reports on two unusual expressions of Michael-based reactivity of 1, as well as an
improved procedure for preparing it.
Results and Discussion
The first observation was that the final key dehydroiodination step of the synthesis (details in
experimental) invariably gave quantities of a by-product 3, the amount depending on work-up
and isolation procedure, Scheme 1.