从乳酸乙酯溶液中直接沉淀3-甲基吡啶多[2,3-b]吡嗪-2(1H)- 1和2-甲基吡啶多[3,4-b]吡嗪-3(4H)- 1的绿色方法

Nicolas Elia, Eric D. Helms
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引用次数: 0

摘要

绿色合成吡啶吡嗪酮的方法是由于它们在设计治疗性化合物中作为支架的用途而发展起来的。优化了乳酸乙酯水溶液的反应条件,通过直接沉淀法使收率最大化。2-甲基吡啶多[2,3-b]吡嗪-2(1H)- 1和2-甲基吡啶多[3,4-b]吡嗪-3(4H)- 1两个关键支架的产率分别为88%和85%。使用92:8和99:1乳酸乙酯:水的混合物,后者在35°C下含有1.5 mol%乳酸,获得了最高的收率。这些结果与使用无水氯仿的传统合成相当,但提供了一种更可持续的替代方法,避免了有害溶剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

A green method for the direct precipitation of 3-methylpyrido[2,3-b]pyrazin-2(1H)-one and 2-methylpyrido[3,4-b]pyrazin-3(4H)-one from ethyl lactate solutions

A green method for the direct precipitation of 3-methylpyrido[2,3-b]pyrazin-2(1H)-one and 2-methylpyrido[3,4-b]pyrazin-3(4H)-one from ethyl lactate solutions
Green methods for synthesizing pyridopyrazinones were developed due to their usefulness as scaffolds in the design of therapeutic compounds. Reaction conditions using aqueous ethyl lactate solutions were optimized to maximize yields through direct product precipitation. Two key scaffolds, 3-methylpyrido[2,3-b]pyrazin-2(1H)-one and 2-methylpyrido[3,4-b]pyrazin-3(4H)-one, were obtained in yields of 88 % and 85 %, respectively. The highest yields were achieved using 92:8 and 99:1 ethyl lactate:water mixtures, with the latter including 1.5 mol% lactic acid at 35 °C. These results are comparable to traditional syntheses using anhydrous chloroform but offer a more sustainable alternative by avoiding hazardous solvents.
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