Solid phase synthesis of tetrahydropyrazine-2-ones by intramolecular Mitsunobu reactions

被引:26
作者
Kung, PP [1 ]
Swayze, E [1 ]
机构
[1] ISIS Pharmaceut, Ibis Therapeut, Carlsbad, CA 92008 USA
关键词
D O I
10.1016/S0040-4039(99)01102-8
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A novel route for the synthesis of tetrahydropyrazine-2-ones on solid support through intramolecular Mitsunobu reactions is reported. The syntheses employ reductive amination of commercially available amino alcohols to attach them to ArgoGel-MB-CHO resin. Amino acids are then coupled to the derivatized solid support for construction of the ring systems and a Mitsunobu reaction between the activated amino acids and amino alcohols forms the derivatized tetrahydropyrazine-2-one rings. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:5651 / 5654
页数:4
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