Expeditious N-monoalkylation of 1,4,7,10-tetraazacyclododecane (cyclen) via formamido protection

被引:34
作者
Boldrini, V
Giovenzana, GB
Pagliarin, R
Palmisano, G
Sisti, M
机构
[1] Dipartimento Sci Chim Fis & Matemat, I-22100 Como, Italy
[2] Dipartimento Chim Organ & Ind, I-20133 Milan, Italy
[3] Dipartimento Sci Chim Alimentari Farmaceut & Farm, I-28100 Novara, Italy
关键词
D O I
10.1016/S0040-4039(00)01092-3
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The reaction of cyclen 1 with chloral hydrate afforded exclusively 1,4,7-triformylcyclen 2 in high yield; the triprotected macrocycle was easily alkylated with various electrophiles in good to excellent yields. The alkaline removal of the formyl groups provided a selective entry into N-monosubstituted cyclen derivatives. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:6527 / 6530
页数:4
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