The development and preparation of the 2,4-dimethoxybenzyl arylhydrazine (DMBAH) "latent" safety-catch linker: solid phase synthesis of ketopiperazines

被引:10
作者
Berst, F [1 ]
Holmes, AB [1 ]
Ladlow, M [1 ]
机构
[1] Univ Cambridge, Chem Lab, GSK Cambridge Technol Ctr, Cambridge CB2 1EW, England
关键词
D O I
10.1039/b301701j
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The development and preparation of the 2,4-dimethoxybenzyl arylhydrazine (DMBAH) linker 3, a new class of "latent" safety-catch linker which is stable under Mitsunobu alkylation conditions and in the presence of amines and hydrazine, is reported. The utility of the new linker is exemplified by the synthesis of ketopiperazines (MKPs) 24 bearing up to four points of diversity using a cyclitive cleavage approach.
引用
收藏
页码:1711 / 1719
页数:9
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