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Mono- and N 1,N 7-dialkylation of 1,4,7,10-tetraazacyclododecane via silicon protection

✍ Scribed by Roignant, Anna�g; Gardinier, Isabelle; Bernard, H�l�ne; Yaouanc, Jean-Jacques; Handel, Henri

Book ID
120074517
Publisher
The Royal Society of Chemistry
Year
1995
Tongue
English
Weight
234 KB
Volume
12
Category
Article
ISSN
0022-4936

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Expeditious N-monoalkylation of 1,4,7,10
Expeditious N-monoalkylation of 1,4,7,10-tetraazacyclododecane (cyclen) via formamido protection
✍ Vincenzo Boldrini; Giovanni B Giovenzana; Roberto Pagliarin; Giovanni Palmisano; 📂 Article 📅 2000 🏛 Elsevier Science 🌐 French ⚖ 109 KB

The reaction of cyclen 1 with chloral hydrate aorded 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