Practical synthesis of 1-aryl-6-(hydroxymethyl)-2-ketopiperazines via a 6-exo amide-epoxide cyclization

被引:17
作者
Powell, NA [1 ]
Ciske, FL [1 ]
Clay, EC [1 ]
Cody, WL [1 ]
Downing, DM [1 ]
Blazecka, PG [1 ]
Holsworth, DD [1 ]
Edmunds, JJ [1 ]
机构
[1] Pfizer Global Res & Dev, Michigan Labs, Ann Arbor, MI 48105 USA
关键词
D O I
10.1021/ol048235t
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Chiral 1-aryl-6-(hydroxymethyl)-2-ketopiperazines can be prepared via an operationally simple, 6-exo epoxide ring-opening cyclization to form the ketopiperazine C6-N1 bond in high yields and with excellent enantiomeric purity.
引用
收藏
页码:4069 / 4072
页数:4
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