Expeditious N-Monoalkylation of 1,4,7,10-Tetraazacyclododecane (Cyclen) via Formamido Protection

V. BOLDRINI, Giovanni Battista GIOVENZANA, R. PAGLIARIN, G. PALMISANO, M. SISTI

Research output: Contribution to journalArticlepeer-review

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.
Original languageEnglish
Pages (from-to)6527-6530
Number of pages4
JournalTetrahedron Letters
Volume41
Issue number33
DOIs
Publication statusPublished - 2000

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