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
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
收藏
页码:8980 / 8983
页数:4
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