Solid-phase synthesis of 6-sulfonylamino morphinan libraries

被引:0
|
作者
Ohno, H
Kawamura, K
Otake, A
Nagase, H
Tanaka, H
Takahashi, T
机构
[1] Tokyo Inst Technol, Dept Appl Chem, Meguro Ku, Tokyo 1528552, Japan
[2] Toray Industries Ltd, Pharmaceut Res Lab, Dept Med Chem, Kamakura, Kanagawa 2488555, Japan
关键词
opioid; morphinan; solid-phase synthesis; ketones; sulfonamides;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A solid-phase synthesis of 6-sulfonylamino morphinan has been developed. The morphinan derivatives were designed as selective opioid ligands. The sulfonamide moiety was introduced by reductive amination of a ketone on solid phase, followed by sulfonylation of the resulting amine. Using this methodology, the synthesis of three combinatorial libraries was accomplished to prepare 339 morphinan derivatives with over 70% purity.
引用
收藏
页码:93 / 96
页数:4
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