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

V Boldrini, GB Giovenzana, R Pagliarin, G Palmisano…

文献索引：Boldrini; Giovenzana; Pagliarin; Palmisano; Sisti Tetrahedron Letters, 2000 , vol. 41, # 33 p. 6527 - 6530

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被引用次数: 35

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.