Pergamon
Tetrahedron Letters, Vol. 38, No. 32, pp. 5631-5634, 1997
© 1997 ElsevierScienceLtd
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0040-4039/97 $17.00 + 0.00
PII: S0040-4039(97)01267-7
High Pressure Induced Mukaiyama Type Aidol Reaction
of bis Trimethylsilyl Ketene Acetals
Moncef Bellassoued, *a Emmanuelle Reboul, a Franfoise Dumas *b
sc Univefsit6 de Paris VI,/.aboramire de Synthtas O~maa~alliqee associd au CNRS,
Tour 45; 4, place Jussieu, 75252 Paris Cedex 05, FRANCE
b: Cealre d'Etades Phamutceutiques, Universit~ de Paris Sad, ~ de Synth~ Oqcmique,
asscci6 au CNRS, 5¢ne J.-B. Ci6nlelit.92296 ChAleamy-Mala&y Cedex. FRANCE
Abstract." The Makaiyama type aldel reaction of his trimcthylsilyl ketene acetals 3 was investigated
under high pressure conditions. Silyl aldois $ were oblained with a syn stereoselectivity, signifa?antly
correlated upon the stedc bulk of R substitnent. In the case of unsaturated bis trimethylsilyl ketene
acelal 4, a pressuredependance of the regioselectivity was observed, the desiredlinearadducts g being
formed at lower pressure. © 1997 Elsevier Science Ltd.
The Mukaiyama aldol reaction of silyl enol ethers I and silyl ketene acetals 2 is recognized as an important
reaction in modem synthetic chemistry, normally carried out in the presence of acids or bases as catalyst) The
success of this procedure hinges on the fact that the reactions are carried out in such a way that the newly formed
aldol is trapped as a neutral silyl compound and is thus protected from wasteful side reactions, particularly from
dissociation into the free carbonyl components which could in turn undergo non selective condensation. One of
us has established that his trimethylsilyl ketene acetals 3 reacted efficiently and stereoseleetively under these
conditions. 2a
OTMS OTMS OTMS
° 0
1 2 3
In connection with our work on the total synthesis of refinoids, 3 we were interested in the high pressure
induced aldol condensation of bis silyl ketene acetals 4, allowing a rapid assembly of the polyene units of these
biomolccules.
R R R OTMS
Ar~-~,~tY , Ar-CHO + ~OTMS
Y = COOTMS, COOH 4
R = H, alkyl
Indeed, Yamamoto 4 reported the high pressure activation of such reaction, using silyl enol ethers 1. Three
imlxaxant points were observed: (1) the reaction proceeds without catalyst even at room temperature; (2)the
a FAX: 01 44 27 30 67 b E-mail: francoise.dumas@cep.u-psud.fr
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