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Asymmetric bridging annulation reaction involving the intramolecular conjugate addition of chiral imines to enoates: Access to a polycyclic system related to the taxane core

✍ Scribed by Christian Cavé; Sophie Boggero; Ramon Casas; Françoise Dumas; Jacqueline Mahuteau; Jean d'Angelo


Publisher
Elsevier Science
Year
1995
Tongue
English
Weight
232 KB
Volume
6
Category
Article
ISSN
0957-4166

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✦ Synopsis


R )-l-phenylethylamine-induced cyclization of ketoenoate 2 4 led to a 2:1 mixture of "all-cis" polycyclic adducts 2 5 and 2 6, structurally related to the taxane series.

Ten years ago, we reported that chiral imines 3, derived from racemic 2-alkylcyclanones 1 and optically active 1-phenylethylamine 2, add, under neutral conditions, to electrophilic alkenes 4 leading, after hydrolytic work-up, to 2,2-dialkylcyclanones 5 with a good yield and excellent regio-and stereoselectivity. 2

4

~ EWG