Issue in Honor of Prof. James M. Cook ARKIVOC 2010 (iv) 74-89
Synthesis of 1-substituted cis-bicyclo[3.3.0]octane-3,7-dione
derivatives as potential precursors of polyquinanes
Pelayo Camps,* José A. Fernández, and Santiago Vázquez
Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmacia,
Universitat de Barcelona, Av. Diagonal 643, E-08028, Barcelona, Spain
E-mail: camps@ub.edu
Dedicated to Prof. James Cook on the occasion of his 65
th
anniversary
Abstract
The synthesis of several 1-substituted cis-bicyclo[3.3.0]octane-3,7-dione derivatives as potential
precursors of a triquinacene having a pyramidalized C=C bond from ethyl cis-3,7-dioxobicyclo-
[3.3.0]octane-1-carboxylate is described.
Keywords: 1-Substituted cis-bicyclo[3.3.0]octane-3,7-diones, polycyclic compounds, cis-
dihydroxylation, Swern oxidation, epoxidation, alkylation
Introduction
For several years, we have been working on the generation, trapping and dimerization of highly
pyramidalized alkenes containing the skeleton of tricyclo[3.3.0.0
3,7
]oct-1(5)-ene 2.
1
These
alkenes are very reactive and can not be isolated, but they can be trapped as Diels-Alder adducts
with various dienophiles. In the absence of a dienophile, these pyramidalized alkenes usually
dimerize in a [2+2] cycloaddition to give cyclobutane dimers 3, which under the standard
reaction conditions of their generation (molten sodium in boiling 1,4-dioxane) are transformed
into diene dimers 4 (Scheme 1).
R
R
R
R
R
R
I
I
R
R
R
R
(i)
(i)
(ii)
R = H, Me
R,R = CH
2
OCH
2
, CH
2
OC(CH
3
)
2
OCH
2
R
R
1 2 3 4
Scheme 1. Generation and dimerization of pyramidalized bicyclo[3.3.0.0
3,7
]oct-1(5)-ene
derivatives 2. (i) Molten Na, 1,4-dioxane, reflux, 3 h. (ii) n-Pentane, hν, 6 h.
ISSN 1551-7012 Page 74
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