1,3,5-trisubstituted 1,4-diazepin-2-ones

被引：16

作者：

Iden, Hassan S. ^{[1
]}

Lubells, William D. ^{[1
]}

机构：

[1] Univ Montreal, Dept Chim, Montreal, PQ H3C 3J7, Canada

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2007年 / 72卷 / 23期

关键词：

D O I：

10.1021/jo701467d

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] Six 1,3,5-trisubstituted 1,4-diazepin-2-ones were synthesized by a sequence featuring the cascade addition of vinyl Grignard to N-[Boc-aminoacyl]-N-alkyl-beta-amino esters, followed by Boc group removal and annulation by a reductive amination. Relative to the parent sequence employing N-Bocaminoacyl beta-amino esters to make 3,5-disubstituted heterocycle, the additional N-alkyl substituent caused a noticeable acceleration and gave relatively higher yield in the 1,4diazepin-2-one annulation.

引用

页码：8980 / 8983

页数：4

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