Versatile solid-phase synthesis of secondary amines from alcohols.: Development of an N-Boc-(o-nitrobenzene)sulfonamide linker

被引:9
作者
Congreve, MS
Kay, C
Scicinski, JJ
Ley, SV
Williams, G
Murray, PJ
McKeown, SC
Watson, SP
机构
[1] Univ Cambridge, GlaxoSmithKline, Cambridge CB2 1EW, England
[2] Univ Cambridge, Dept Chem, Cambridge CB2 1EW, England
[3] OSI Pharmaceut, Oxford OX4 6LT, England
[4] GlaxoSmithKline, Stevenage SG1 2NY, Herts, England
关键词
D O I
10.1016/S0040-4039(03)00574-4
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The development of a versatile amine releasing linker based on the modified o-nitrobenzene sulfonamide protective group is described. This new N-Boc-o-nitrobenzenesulfonamide (Boc-ONBS) linker enables the elaboration on resin of primary and secondary amines by sequential substitution of the sulfonamide moiety using the Mitsunobu reaction. A 16-member array of secondary and Boc protected primary amines was then prepared using this linker. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:4153 / 4156
页数:4
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