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

✍ Scribed by Vincenzo Boldrini; Giovanni B Giovenzana; Roberto Pagliarin; Giovanni Palmisano; Massimo Sisti

• Book ID: 104210695
• Publisher: Elsevier Science
• Year: 2000
• Tongue: French
• Weight: 109 KB
• Volume: 41
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(00)01092-3

✦ Synopsis

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 cyclen derivatives.