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Strategies and Synthetic Methods Directed Toward the Preparation of Libraries of Substituted Isoquinolines
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2010-07-22 00:00:00 , DOI: 10.1021/jo100980p
Emelia Awuah 1 , Alfredo Capretta 1
Affiliation  

Strategies for the production of substituted isoquinoline libraries were developed and explored. Routes involving microwave-assisted variants of the Bischler−Napieralski or Pictet−Spengler reaction allowed for cyclization of substituted β-arylethylamine derivatives. The dihydroisoquinolines and tetrahydroisoquinolines thus generated could then be oxidized to their corresponding isoquinoline analogues. An alternate strategy, however, involving the preparation and activation of isoquinolin-1(2H)-ones is demonstrated to be a more practical, rapid, and efficient route to C1- and C4-substituted isoquinoline libraries.

中文翻译:

取代异喹啉文库制备的策略和综合方法

开发和探索了取代异喹啉文库的生产策略。涉及Bischler-Napieralski或Pictet-Spengler反应的微波辅助变体的途径可实现取代的β-芳基乙胺衍生物的环化。然后可以将由此产生的二氢异喹啉和四氢异喹啉氧化为它们相应的异喹啉类似物。然而,另一种涉及制备和激活异喹啉-1(2 H)-ones的策略被证明是一种更实用,快速,有效的通往C1和C4取代异喹啉文库的途径。
更新日期:2010-07-22
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