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以多样性为导向的全合成 (DOTS) 的pyridoquinazolinone类化合物及其类似物

Sivappa Rasapalli¹, Yanchang Huang¹, Vamshikrishna Reddy Sammeta¹

¹Department of Chemistry and Biochemistry, University of Massachusetts Dartmouth, 285 Old Westport Rd, North Dartmouth, MA-02747, USA.

Tetrahedron chem

|September 27, 2024

概括

一个简短的以多样性为导向的总合成 (DOTS) 提供了复杂的类化合物,如鲁特卡尔宾及其类似物. 这种高效的方法利用一个关键的三环中间体来构建多样化的分子支架.

科学领域:

有机化学有机化学
合成化学合成化学
药用化学医学化学

背景情况:

鲁他卡和相关的化物表现出显著的生物活性.
开发高效的合成路径到这些复杂的天然产品对于进一步的研究至关重要.

研究的目的:

为了实现替代的鲁他卡和相关类的短期多样性导向总合成 (DOTS).
从简单的原材料建立一个高效的合成策略.

主要方法:

合成使用了一个关键的三环中间体,mackinazolindione.
关键反应包括氨基酸和乙氧化与石酸的合,然后进行迪克曼凝结.
多样性是通过修改三环原子核来引入的.

主要成果:

成功合成了替代的鲁特卡尔宾,homo-luotonins,homo-vasicinone,homo-isaindigotones和homo-vasnetine的替代物.
这种合成是在短时间内从易于获得的前体中完成的.
关键的三环基中间体得到了高效的制备.

结论:

开发的DOTS策略对于访问一系列复杂的化物结构是有效的.
这种方法为合成新型鲁他卡类同类药物提供了一个有价值的平台.
该研究强调了迪克曼凝结在构建多环系统中的实用性.

关键词:

亚萨 - 鲁塔埃卡尔宾 (aza-rutaecarpine) 是一种葡萄糖.面向多样性的综合总结人类 - 卢托尼尼.在Homo-vasicinone中使用.皮里多基纳索利诺 (Pyridoquinazolinone) 是一种氨酸.

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