Expeditious N-monoalkylation of 1, 4, 7, 10-tetraazacyclododecane (cyclen) via formamido protection
V Boldrini, GB Giovenzana, R Pagliarin, G Palmisano…
Index: Boldrini; Giovenzana; Pagliarin; Palmisano; Sisti Tetrahedron Letters, 2000 , vol. 41, # 33 p. 6527 - 6530
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Citation Number: 35
Abstract
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.
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