A new cleavage strategy for the solid-phase synthesis of secondary amines

被引：54

作者：

Conti, P ^{[1
]}

Demont, D ^{[1
]}

Cals, J ^{[1
]}

Ottenheijm, HCJ ^{[1
]}

Leysen, D ^{[1
]}

机构：

[1] NV ORGANON,SCI DEV GRP,DEPT MED CHEM,NL-5340 BH OSS,NETHERLANDS

来源：

TETRAHEDRON LETTERS | 1997年 / 38卷 / 16期

关键词：

D O I：

10.1016/S0040-4039(97)00502-9

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The clean and efficient cleavage of N-benzyl linked tertiary amines from a solid support (e.g. 4) by treatment with alpha-chloroethyl chloroformate (ACE-Cl)/methanol to yield secondary amines 7 is described. This allows the solid-phase synthetic transformation of the secondary amine 2 into 7. When the Merrifield resin 1 is used the N-tethered amine-polymeric matrix ensemble is stable towards a wide variety of reaction conditions. (C) 1997 Published by Elsevier Science Ltd.

引用

页码：2915 / 2918

页数：4

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