Polymer-supported synthesis of diverse perhydro-1,4-diazepine-2,5-diones

被引：23

作者：

Krchnak, V ^{[1
]}

Weichsel, AS ^{[1
]}

机构：

[1] SELECTIDE CORP,TUCSON,AZ 85737

来源：

TETRAHEDRON LETTERS | 1997年 / 38卷 / 42期

关键词：

D O I：

10.1016/S0040-4039(97)01772-3

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The chemistry, synthesis of model compounds, selection of building blocks, and synthesis of a library of 1,4,7-trisubstituted perhydro-1,4-diazepine-2,5-diones are described. Secondary diamines and Fmoc protected amino alcohols were attached to chlorotrityl resin and the amino group acylated with Fmoc-Asp(OAll). The Fmoc group was cleaved, and the amino group alkylated. Then bromoacetic acid was coupled to the amino group and the bromide displaced by primary amines. After removal of the allyl ester function, the seven membered ring was closed upon mild activation of the carboxyl group. Products were cleaved from the resin by TFA vapor. (C) 1997 Elsevier Science Ltd.

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页码：7299 / 7302

页数：4

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