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Comparative routes to 7-carboxymethyl-pterin: A useful medicinal chemistry building block
Pteridines ( IF 0.4 ) Pub Date : 2022-01-01 , DOI: 10.1515/pteridines-2022-0036
Zachary Bennett 1 , Kassidy Grumbles 1 , Jeffrey Pruet 1
Affiliation  

Pterins, such as folate and biopterin, and their derivatives hold significant importance given their biological relevance, as well as the numerous pterin-based inhibitors developed for targeting various biological targets. For this reason, pterins can be viewed as a privileged scaffold , as the discovery of new pterin analogs gives rise to a vast array of potential drug candidates. 7-carboxymethyl-pterin (7-CMP) represents a useful scaffold for the rapid generation of structurally diverse pterin amides and has been a key building block in medicinal chemistry. In an effort to facilitate rapid generation of this pterin scaffold, we have explored multiple routes towards 7-CMP to assess the most efficient method of generation. Methods were evaluated based on yield, regioselectivity, reaction time, and hazardous reaction conditions. This work can aide in the synthesis and discovery of new pterin-based drug candidates.

中文翻译:

7-羧甲基蝶呤的比较路线:一种有用的药物化学构件

蝶呤,如叶酸和生物蝶呤,以及它们的衍生物,鉴于它们的生物学相关性,以及为靶向各种生物靶点而开发的众多基于蝶呤的抑制剂,具有重要意义。出于这个原因,蝶呤可以被视为一种特殊的支架,因为新蝶呤类似物的发现产生了大量潜在的候选药物。7-羧甲基蝶呤 (7-CMP) 代表了一种有用的支架,可用于快速生成结构多样的蝶呤酰胺,并且一直是药物化学中的关键组成部分。为了促进这种蝶呤支架的快速生成,我们探索了多种通往 7-CMP 的途径,以评估最有效的生成方法。基于产率、区域选择性、反应时间和危险反应条件评估方法。
更新日期:2022-01-01
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