在 (+) -安菲迪诺化物t1的全合成过程中,对 (+) -安菲迪诺化物t1进行了选择
1Department of Chemistry, University of Illinois at Chicago, 845 West Taylor Street, Chicago, IL 60607, USA. arunghos@uic.edu
Journal of the American Chemical Society
|February 27, 2003
概括
研究人员报告了第一个安菲迪诺利德T1的全合成,这是一种强大的抗瘤宏化物. 这种复杂的分子是使用融合策略和关键的立体选择反应组装的.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 自然产品的合成自然产品的合成
背景情况:
- 安菲迪诺利德T1是一种从Amphidinium sp.中分离出来的19个成员的大化物.
- 它对各种国家癌症研究所 (NCI) 瘤细胞系表现出强大的抗瘤特性.
研究的目的:
- 为了实现第一个enantioselective总合成的安菲迪诺利德T1.1.
- 开发一种融合合成策略,用于构建这个复杂的宏观体.
主要方法:
- 融合合成涉及C1-C10和C11-C21碎片.
- 氧化碳离子介导的化和山口巨乳化.
- 交叉转化,化和易斯酸催化化.
- 通过乙烯酸乙烯酸介导的-阿尔多尔反应.
- 保护敏感的功能组作为乙烯衍生物.
主要成果:
- 成功进行了 (+) - 氨基氨基化物T1.1的酶选择性总合成.
- 使用先进的合成方法有效地构建关键片段.
- 多个性中心的立体选择性形成.
结论:
- 描述的合成途径提供了对安菲迪诺利德T1.1的获取.
- 综合强调了用于复杂天然产品合成的方法的实用性.
- 这项工作为进一步的生物评估和模拟开发奠定了基础.
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