Synthesis

A short enantioselective synthesis of the topoisomerase II inhibitor (+)-eleutherin

JS Gibson, O Andrey, MA Brimble

文献索引：Gibson, Jennifer S.; Andrey, Olivier; Brimble, Margaret A. Synthesis, 2007 , # 17 p. 2611 - 2613

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摘要

We therefore envisaged a more efficient, alternate route to (+)-eleutherin 1, proceeding via the intermediate naphthalene 2, which we planned to access via a Hauser-Kraus annulation [7] of known cyanophthalide 3 [8] with chiral α,β-unsaturated ketone 4, followed by reductive methylation of the resulting naphthoquinone (Scheme [1] ). ... Cyanophthalide 3 was readily prepared from 2-methoxybenzoic acid (5) by conversion to the corresponding N,N-diethylbenzamide, ...