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. (C) 2000 Elsevier Science Ltd. All rights reserved.
Expeditious N-monoalkylation of 1,4,7,10-tetraazacyclododecane (cyclen) via formamido protection / V. Boldrini, G. Giovenzana, R. Pagliarin, G. Palmisano, M. Sisti. - In: TETRAHEDRON LETTERS. - ISSN 0040-4039. - 41:33(2000), pp. 6527-6530.
Expeditious N-monoalkylation of 1,4,7,10-tetraazacyclododecane (cyclen) via formamido protection
R. Pagliarin;
2000
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. (C) 2000 Elsevier Science Ltd. All rights reserved.
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