A traceless solid-phase synthesis of 2-imidazolones

被引：15

作者：

Cheng, JF ^{[1
]}

Kaiho, C ^{[1
]}

Chen, M ^{[1
]}

Arrhenius, T ^{[1
]}

Nadzan, A ^{[1
]}

机构：

[1] LLC, Chugai Pharm USA, Dept Chem, San Diego, CA 92121 USA

来源：

TETRAHEDRON LETTERS | 2002年 / 43卷 / 26期

关键词：

2-imidazolone; traceless linker; solid-phase organic synthesis;

D O I：

10.1016/S0040-4039(02)00897-3

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A traceless solid-phase synthesis of 2-imidazolones has been developed. Poly-mer-bound glycerol resin was reacted with bromoacetaldehyde diethyl acetal to give the cyclic acetal bromide on the solid support. Amination of the rein-bound acetal bromide followed by urea formation by reaction with isocyanates afforded the resin-bound urea acetals. The aldehyde urea intermediate, which was released from the resin upon treatment with TEA, immediately cyclized to afford the desired 2-imidazolones in good yield and purity. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：4571 / 4573

页数：3

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