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Stereodivergent approach to Alzheimer's therapeutic agent (R)-(−) and (S)-(+)-arundic acid employing chiral 4-pentenol derivatives as building blocks
Tetrahedron ( IF 2.1 ) Pub Date : 2017-03-05 16:35:58
Viraj A. Bhosale, Suresh B. Waghmode

An efficient stereodivergent total synthesis of anti-Alzheimer agent (R)-(−) and (S)-(+)-arundic acid has been achieved from both chiral and nonchiral materials. This strategy features an efficient approach to separable diastereomeric C-2 chiral 4-pentenol intermediates employing proline catalysed asymmetric α-aminooxylation and [3,3] sigmatropic Claisen rearrangement are the highlights of present synthesis.

中文翻译:

以手性4-戊烯醇衍生物为结构单元的阿尔茨海默氏病治疗剂(R)-(-)和(S)-(+)-金刚烷酸的立体发散方法

从手性和非手性材料都已经实现了抗阿尔茨海默病剂(R)-(-)和(S)-(+)-金刚烷酸的有效立体发散性全合成。该策略的特征是采用脯氨酸催化的不对称α-氨基氧基化和[3,3]σ克莱森重排的可分离非对映体C-2手性4-戊烯醇中间体的有效方法是本合成的重点。
更新日期:2017-03-06
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