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

来源：

SYNLETT | 2002年 / 01期

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

页码：93 / 96

页数：4

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