Synthesis of N-alkyl-octahydroisoquinolin-1-one-8-carboxamide libraries using a Tandem Diels-Alder/Acylation sequence

Synthesis of N-alkyl-octahydroisoquinolin-1-one-8-carboxamide libraries using a Tandem Diels-Alder/Acylation sequence
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DOI:
10.1021/cc700127f
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发表时间:
2007-11-01
影响因子:
--
通讯作者:
Aube, Jeffrey
Aube, Jeffrey
中科院分区:
其他
文献类型:
--
作者:
Frankowski, Kevin J.;Hirt, Erin E.;Aube, Jeffrey

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开发了一种合成序列,其中含有连接的仲胺的二烯与马来酸酐反应,一步得到标题结构。该反应涉及与酰亚胺基团的转酰化反应组合的Diels-Alder反应。使用这种方法构建了一系列的六个支架。每个支架随后与12种胺反应,得到包含72种化合物的库。
A synthetic sequence was developed in which a diene containing an attached secondary amine was reacted with maleic anhydride to afford the title structures in one step. The reaction involves a, Diels-Alder reaction combined with a transacylation reaction of the imide group. A series of six scaffolds was constructed using this methodology. Each scaffold was subsequently reacted with 12 amines to afford a library containing 72 compounds.