对羟基赫曲霉素A的不对称、立体控制全合成。
Asymmetric, stereocontrolled total synthesis of paraherquamide A.
作者信息
Williams Robert M, Cao Jianhua, Tsujishima Hidekazu, Cox Rhona J
机构信息
Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA.
出版信息
J Am Chem Soc. 2003 Oct 8;125(40):12172-8. doi: 10.1021/ja036713+.
The first total synthesis of paraherquamide A, a potent anthelmintic agent isolated from various Penicillium sp. with promising activity against drug-resistant intestinal parasites, is reported. Key steps in this asymmetric, stereocontrolled total synthesis include a new enantioselective synthesis of alpha-alkylated-beta-hydroxyproline derivatives to access the substituted proline nucleus and a highly diastereoselective intramolecular S(N)2' cyclization to generate the core bicyclo[2.2.2]diazaoctane ring system.
据报道，首次全合成了对驱虫酰胺A，它是从多种青霉菌中分离出的一种强效驱虫剂，对耐药肠道寄生虫具有良好的活性。这种不对称、立体控制的全合成中的关键步骤包括一种新的对映选择性合成α-烷基化-β-羟基脯氨酸衍生物以构建取代脯氨酸核，以及一种高度非对映选择性的分子内S(N)2'环化反应以生成核心双环[2.2.2]二氮杂辛烷环系。
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